General Information of the Protein
Protein ID
PT01378
Protein Name
Leucine-rich repeat serine/threonine-protein kinase 2
Secondarily
Protein Name
Dardarin
Gene Name
LRRK2
Secondarily
Gene Name
PARK8
Sequence
MASGSCQGCEEDEETLKKLIVRLNNVQEGKQIETLVQILEDLLVFTYSERASKLFQGKNIHVPLLIVLDSYMRVASVQQVGWSLLCKLIEVCPGTMQSLMGPQDVGNDWEVLGVHQLILKMLTVHNASVNLSVIGLKTLDLLLTSGKITLLILDEESDIFMLIFDAMHSFPANDEVQKLGCKALHVLFERVSEEQLTEFVENKDYMILLSALTNFKDEEEIVLHVLHCLHSLAIPCNNVEVLMSGNVRCYNIVVEAMKAFPMSERIQEVSCCLLHRLTLGNFFNILVLNEVHEFVVKAVQQYPENAALQISALSCLALLTETIFLNQDLEEKNENQENDDEGEEDKLFWLEACYKALTWHRKNKHVQEAACWALNNLLMYQNSLHEKIGDEDGHFPAHREVMLSMLMHSSSKEVFQASANALSTLLEQNVNFRKILLSKGIHLNVLELMQKHIHSPEVAESGCKMLNHLFEGSNTSLDIMAAVVPKILTVMKRHETSLPVQLEALRAILHFIVPGMPEESREDTEFHHKLNMVKKQCFKNDIHKLVLAALNRFIGNPGIQKCGLKVISSIVHFPDALEMLSLEGAMDSVLHTLQMYPDDQEIQCLGLSLIGYLITKKNVFIGTGHLLAKILVSSLYRFKDVAEIQTKGFQTILAILKLSASFSKLLVHHSFDLVIFHQMSSNIMEQKDQQFLNLCCKCFAKVAMDDYLKNVMLERACDQNNSIMVECLLLLGADANQAKEGSSLICQVCEKESSPKLVELLLNSGSREQDVRKALTISIGKGDSQIISLLLRRLALDVANNSICLGGFCIGKVEPSWLGPLFPDKTSNLRKQTNIASTLARMVIRYQMKSAVEEGTASGSDGNFSEDVLSKFDEWTFIPDSSMDSVFAQSDDLDSEGSEGSFLVKKKSNSISVGEFYRDAVLQRCSPNLQRHSNSLGPIFDHEDLLKRKRKILSSDDSLRSSKLQSHMRHSDSISSLASEREYITSLDLSANELRDIDALSQKCCISVHLEHLEKLELHQNALTSFPQQLCETLKSLTHLDLHSNKFTSFPSYLLKMSCIANLDVSRNDIGPSVVLDPTVKCPTLKQFNLSYNQLSFVPENLTDVVEKLEQLILEGNKISGICSPLRLKELKILNLSKNHISSLSENFLEACPKVESFSARMNFLAAMPFLPPSMTILKLSQNKFSCIPEAILNLPHLRSLDMSSNDIQYLPGPAHWKSLNLRELLFSHNQISILDLSEKAYLWSRVEKLHLSHNKLKEIPPEIGCLENLTSLDVSYNLELRSFPNEMGKLSKIWDLPLDELHLNFDFKHIGCKAKDIIRFLQQRLKKAVPYNRMKLMIVGNTGSGKTTLLQQLMKTKKSDLGMQSATVGIDVKDWPIQIRDKRKRDLVLNVWDFAGREEFYSTHPHFMTQRALYLAVYDLSKGQAEVDAMKPWLFNIKARASSSPVILVGTHLDVSDEKQRKACMSKITKELLNKRGFPAIRDYHFVNATEESDALAKLRKTIINESLNFKIRDQLVVGQLIPDCYVELEKIILSERKNVPIEFPVIDRKRLLQLVRENQLQLDENELPHAVHFLNESGVLLHFQDPALQLSDLYFVEPKWLCKIMAQILTVKVEGCPKHPKGIISRRDVEKFLSKKRKFPKNYMSQYFKLLEKFQIALPIGEEYLLVPSSLSDHRPVIELPHCENSEIIIRLYEMPYFPMGFWSRLINRLLEISPYMLSGRERALRPNRMYWRQGIYLNWSPEAYCLVGSEVLDNHPESFLKITVPSCRKGCILLGQVVDHIDSLMEEWFPGLLEIDICGEGETLLKKWALYSFNDGEEHQKILLDDLMKKAEEGDLLVNPDQPRLTIPISQIAPDLILADLPRNIMLNNDELEFEQAPEFLLGDGSFGSVYRAAYEGEEVAVKIFNKHTSLRLLRQELVVLCHLHHPSLISLLAAGIRPRMLVMELASKGSLDRLLQQDKASLTRTLQHRIALHVADGLRYLHSAMIIYRDLKPHNVLLFTLYPNAAIIAKIADYGIAQYCCRMGIKTSEGTPGFRAPEVARGNVIYNQQADVYSFGLLLYDILTTGGRIVEGLKFPNEFDELEIQGKLPDPVKEYGCAPWPMVEKLIKQCLKENPQERPTSAQVFDILNSAELVCLTRRILLPKNVIVECMVATHHNSRNASIWLGCGHTDRGQLSFLDLNTEGYTSEEVADSRILCLALVHLPVEKESWIVSGTQSGTLLVINTEDGKKRHTLEKMTDSVTCLYCNSFSKQSKQKNFLLVGTADGKLAIFEDKTVKLKGAAPLKILNIGNVSTPLMCLSESTNSTERNVMWGGCGTKIFSFSNDFTIQKLIETRTSQLFSYAAFSDSNIITVVVDTALYIAKQNSPVVEVWDKKTEKLCGLIDCVHFLREVMVKENKESKHKMSYSGRVKTLCLQKNTALWIGTGGGHILLLDLSTRRLIRVIYNFCNSVRVMMTAQLGSLKNVMLVLGYNRKNTEGTQKQKEIQSCLTVWDINLPHEVQNLEKHIEVRKELAEKMRRTSVE
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TKL protein kinase group
>
TKL protein kinase LRRK family
Function
Serine/threonine-protein kinase which phosphorylates a broad range of proteins involved in multiple processes such as neuronal plasticity, innate immunity, autophagy, and vesicle trafficking (PubMed:20949042, PubMed:22012985, PubMed:26824392, PubMed:27830463, PubMed:29125462, PubMed:28720718, PubMed:29127255, PubMed:30398148, PubMed:29212815, PubMed:30635421, PubMed:21850687, PubMed:23395371, PubMed:17114044, PubMed:24687852, PubMed:26014385, PubMed:25201882). Is a key regulator of RAB GTPases by regulating the GTP/GDP exchange and interaction partners of RABs through phosphorylation (PubMed:26824392, PubMed:28720718, PubMed:29127255, PubMed:30398148, PubMed:29212815, PubMed:29125462, PubMed:30635421). Phosphorylates RAB3A, RAB3B, RAB3C, RAB3D, RAB5A, RAB5B, RAB5C, RAB8A, RAB8B, RAB10, RAB12, RAB35, and RAB43 (PubMed:26824392, PubMed:28720718, PubMed:29127255, PubMed:30398148, PubMed:29212815, PubMed:29125462, PubMed:30635421, PubMed:23395371). Regulates the RAB3IP-catalyzed GDP/GTP exchange for RAB8A through the phosphorylation of 'Thr-72' on RAB8A (PubMed:26824392). Inhibits the interaction between RAB8A and GDI1 and/or GDI2 by phosphorylating 'Thr-72' on RAB8A (PubMed:26824392). Regulates primary ciliogenesis through phosphorylation of RAB8A and RAB10, which promotes SHH signaling in the brain (PubMed:29125462, PubMed:30398148). Together with RAB29, plays a role in the retrograde trafficking pathway for recycling proteins, such as mannose-6-phosphate receptor (M6PR), between lysosomes and the Golgi apparatus in a retromer-dependent manner (PubMed:23395371). Regulates neuronal process morphology in the intact central nervous system (CNS) (PubMed:17114044). Plays a role in synaptic vesicle trafficking (PubMed:24687852). Plays an important role in recruiting SEC16A to endoplasmic reticulum exit sites (ERES) and in regulating ER to Golgi vesicle-mediated transport and ERES organization (PubMed:25201882). Positively regulates autophagy through a calcium-dependent activation of the CaMKK/AMPK signaling pathway (PubMed:22012985). The process involves activation of nicotinic acid adenine dinucleotide phosphate (NAADP) receptors, increase in lysosomal pH, and calcium release from lysosomes (PubMed:22012985). Phosphorylates PRDX3 (PubMed:21850687). By phosphorylating APP on 'Thr-743', which promotes the production and the nuclear translocation of the APP intracellular domain (AICD), regulates dopaminergic neuron apoptosis (PubMed:28720718). Acts as a positive regulator of innate immunity by mediating phosphorylation of RIPK2 downstream of NOD1 and NOD2, thereby enhancing RIPK2 activation (PubMed:27830463). Independent of its kinase activity, inhibits the proteasomal degradation of MAPT, thus promoting MAPT oligomerization and secretion (PubMed:26014385). In addition, has GTPase activity via its Roc domain which regulates LRRK2 kinase activity (PubMed:18230735, PubMed:26824392, PubMed:29125462, PubMed:28720718, PubMed:29212815).
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Uniprot ID
Primary ID:
Q5S007

Secondarily ID:
A6NJU2
Q6ZS50
Q8NCX9
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Ensembl ID
ENSG00000188906
HGNC ID
HGNC:18618
Subcellular Location
Cytoplasmic vesicle
Perikaryon
Golgi apparatus membrane
Cell projection
Axon
Cell projection
Dendrite
Endoplasmic reticulum membrane
Cytoplasmic vesicle
Secretory vesicle
Synaptic vesicle membrane
Endosome
Lysosome
Mitochondrion outer membrane
Cytoplasm
Cytoskeleton
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0572904
(5S)-5-[[3-(2-morpholin-4-ylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C27H26N6O
 2
1
EC50 = 17 nM
   TI
   LI
   LO
   TS
2
EC50 = 260 nM
   TI
   LI
   LO
   TS
CP0546499
(5S)-5-[[3-(2,6-dimethylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C25H23N5
 2
1
EC50 = 20 nM
   TI
   LI
   LO
   TS
2
EC50 = 700 nM
   TI
   LI
   LO
   TS
CP0564501
(5S)-5-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C24H21N5
 2
1
EC50 = 20 nM
   TI
   LI
   LO
   TS
2
EC50 = 800 nM
   TI
   LI
   LO
   TS
CP0644312
cis-2,6-Dimethyl-4-(6-(5-(1-methylcyclopropoxy)-1H-indazol-3-yl)pyrimidin-4-yl)morpholine
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C21H25N5O2
 2
1
EC50 = 23 nM
   TI
   LI
   LO
   TS
2
EC50 = 30 nM
   TI
   LI
   LO
   TS
CP0033205
(5R)-5-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C24H21N5
 2
1
EC50 = 40 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0568003
4-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]benzene-1,3-dicarbonitrile
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C21H14N6
 2
1
EC50 = 60 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0218399
4-[[(1R)-1-cyclopropylethyl]amino]-7-pyridin-4-ylcinnoline-3-carboxamide
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C19H19N5O
 1
1
EC50 = 62 nM
   TI
   LI
   LO
   TS
CP0023856
4-[[(1R)-1-cyclopropylethyl]amino]-7-(4-methylsulfonylphenyl)cinnoline-3-carboxamide
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C21H22N4O3S
 1
1
EC50 = 70 nM
   TI
   LI
   LO
   TS
CP0568785
(5R)-5-[[3-(2,6-dimethylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C25H23N5
 2
1
EC50 = 70 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0570264
(5S)-5-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C23H19N5
 2
1
EC50 = 70 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0067767
4-[[(2R)-butan-2-yl]amino]-7-(4-methylsulfonylphenyl)cinnoline-3-carboxamide
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C20H22N4O3S
 1
1
EC50 = 73 nM
   TI
   LI
   LO
   TS
CP0543315
(4R)-4-[[3-(2,6-dimethylpyridin-4-yl)-1H-indazol-5-yl]amino]-3,4-dihydro-2H-chromene-7-carbonitrile
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C24H21N5O
 2
1
EC50 = 90 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0019734
4-(propan-2-ylamino)-6-(1H-pyrazol-4-yl)cinnoline-3-carboxamide
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C15H16N6O
 1
1
EC50 = 109 nM
   TI
   LI
   LO
   TS
CP0579368
(5R)-5-[[3-(2-morpholin-4-ylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C27H26N6O
 2
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0019820
7-(1-methylpyrazol-4-yl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
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C17H17N5
 1
1
EC50 = 140 nM
   TI
   LI
   LO
   TS
CP0033544
2-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]benzonitrile
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C20H15N5
 2
1
EC50 = 150 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0564488
4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-3,4-dihydro-2H-chromene-7-carbonitrile
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C22H17N5O
 2
1
EC50 = 160 nM
   TI
   LI
   LO
   TS
2
EC50 = 30000 nM
   TI
   LI
   LO
   TS
CP0574429
1-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-2,3-dihydro-1H-indene-5-carbonitrile
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C22H17N5
 2
1
EC50 = 200 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0067768
7-(4-methylsulfonylphenyl)-4-(propan-2-ylamino)cinnoline-3-carboxamide
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C19H20N4O3S
 1
1
EC50 = 218 nM
   TI
   LI
   LO
   TS
CP0321712
4-[3-cyano-4-(propan-2-ylamino)quinolin-7-yl]-N-methylbenzenesulfonamide
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C20H20N4O2S
 1
1
EC50 = 226 nM
   TI
   LI
   LO
   TS
CP0022216
4-(propan-2-ylamino)-7-pyridin-4-ylcinnoline-3-carboxamide
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C17H17N5O
 1
1
EC50 = 242 nM
   TI
   LI
   LO
   TS
CP0233613
4-(propan-2-ylamino)-7-(1,2-thiazol-4-yl)cinnoline-3-carboxamide
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C15H15N5OS
 1
1
EC50 = 290 nM
   TI
   LI
   LO
   TS
CP0550091
(5R)-5-[[3-(1-methylpyrazol-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C22H20N6
 2
1
EC50 = 290 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0543316
(5R)-5-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C23H19N5
 2
1
EC50 = 310 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0573657
(4R)-4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-3,4-dihydro-2H-chromene-7-carbonitrile
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C22H17N5O
 2
1
EC50 = 320 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0031119
4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzene-1,3-dicarbonitrile
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C20H12N6
 2
1
EC50 = 370 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0564492
3-fluoro-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H12FN5
 2
1
EC50 = 390 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0077182
7-(4-morpholin-4-ylsulfonylphenyl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
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C23H24N4O3S
 1
1
EC50 = 416 nM
   TI
   LI
   LO
   TS
CP0016537
7-(4-methylsulfonylphenyl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
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C20H19N3O2S
 1
1
EC50 = 435 nM
   TI
   LI
   LO
   TS
CP0114881
4-(azetidin-1-yl)-7-(1-methylpyrazol-4-yl)quinoline-3-carbonitrile
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C17H15N5
 1
1
EC50 = 504 nM
   TI
   LI
   LO
   TS
CP0545147
5-methyl-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C20H15N5
 2
1
EC50 = 530 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0185411
7-(2-methyl-1,3-thiazol-5-yl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
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C17H16N4S
 1
1
EC50 = 545 nM
   TI
   LI
   LO
   TS
CP0568096
N-(2-nitrophenyl)-3-pyridin-4-yl-1H-indazol-5-amine
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C18H13N5O2
 2
1
EC50 = 570 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0572902
2-fluoro-6-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H12FN5
 2
1
EC50 = 620 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0568097
2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H13N5
 2
1
EC50 = 670 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0577522
2-[[3-(2-methoxypyridin-4-yl)-1H-indazol-5-yl]amino]benzonitrile
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C20H15N5O
 2
1
EC50 = 690 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0550120
N-(3,4-dihydro-2H-chromen-4-yl)-3-pyridin-4-yl-1H-indazol-5-amine
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C21H18N4O
 2
1
EC50 = 730 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0019480
4-[[(1R)-1-cyclopropylethyl]amino]-7-[4-(2-oxo-1,3-oxazol-3-yl)phenyl]quinoline-3-carbonitrile
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C24H20N4O2
 1
1
EC50 = 731 nM
   TI
   LI
   LO
   TS
CP0568101
(5R)-5-[(6-fluoro-3-pyridin-4-yl-1H-indazol-5-yl)amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C23H18FN5
 2
1
EC50 = 750 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0550119
(4R)-4-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]-3,4-dihydro-2H-chromene-7-carbonitrile
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C23H19N5O
 2
1
EC50 = 760 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0546879
2-methyl-3-[[(3-pyridin-4-yl-1H-indazol-5-yl)amino]methyl]benzonitrile
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C21H17N5
 2
1
EC50 = 790 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0578424
4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H13N5
 2
1
EC50 = 930 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0577652
3-nitro-4-[(3-pyridin-4-yl-1H-indazol-5-yl)oxy]benzonitrile
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C19H11N5O3
 2
1
EC50 = 1080 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0065744
4-(dimethylamino)-7-(4-methylsulfonylphenyl)quinoline-3-carbonitrile
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C19H17N3O2S
 1
1
EC50 = 1134 nM
   TI
   LI
   LO
   TS
CP0031120
3-nitro-4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H12N6O2
 2
1
EC50 = 1400 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0077181
7-(4-methylsulfonylphenyl)-4-piperidin-1-ylquinoline-3-carbonitrile
   Show/Hide
C22H21N3O2S
 1
1
EC50 = 1599 nM
   TI
   LI
   LO
   TS
CP0262506
7-(6-methylsulfonylpyridin-3-yl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
   Show/Hide
C19H18N4O2S
 1
1
EC50 = 1599 nM
   TI
   LI
   LO
   TS
CP0568098
3-[[(3-pyridin-4-yl-1H-indazol-5-yl)amino]methyl]benzonitrile
   Show/Hide
C20H15N5
 2
1
EC50 = 1700 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0568099
(5R)-5-[[3-(2-methoxypyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
   Show/Hide
C24H21N5O
 2
1
EC50 = 1840 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0065790
7-(5-chlorothiophen-2-yl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
   Show/Hide
C17H14ClN3S
 1
1
EC50 = 2621 nM
   TI
   LI
   LO
   TS
CP0543313
5-fluoro-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C19H12FN5
 2
1
EC50 = 2890 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0546878
5-methoxy-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C20H15N5O
 2
1
EC50 = 3290 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0543311
(5R)-5-[[3-pyridin-4-yl-6-(trifluoromethyl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
   Show/Hide
C24H18F3N5
 2
1
EC50 = 3300 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0546880
5-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]naphthalene-2-carbonitrile
   Show/Hide
C23H15N5
 2
1
EC50 = 6300 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0573659
2-methyl-6-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C20H15N5
 2
1
EC50 = 13000 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0564486
3-methyl-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C20H15N5
 2
1
EC50 = 35000 nM
   TI
   LI
   LO
   TS
2
EC50 = 100000 nM
   TI
   LI
   LO
   TS
CP0564500
3-[(1S)-1-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]ethyl]benzonitrile
   Show/Hide
C21H17N5
 2
1
EC50 = 40000 nM
   TI
   LI
   LO
   TS
2
EC50 = 50000 nM
   TI
   LI
   LO
   TS
CP0573658
3-methoxy-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C20H15N5O
 2
1
EC50 = 49000 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0564491
2-[(3-pyridin-4-yl-1H-indazol-5-yl)oxy]benzonitrile
   Show/Hide
C19H12N4O
 2
1
EC50 = 49800 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0564490
3-methyl-4-[(3-pyridin-4-yl-1H-indazol-5-yl)oxy]benzonitrile
   Show/Hide
C20H14N4O
 2
1
EC50 = 60000 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0550117
4-[[(3-pyridin-4-yl-1H-indazol-5-yl)amino]methyl]benzonitrile
   Show/Hide
C20H15N5
 2
1
EC50 = 80000 nM
   TI
   LI
   LO
   TS
2
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0152600
3-nitro-4-[(2-oxo-1,3-dihydrobenzimidazol-5-yl)amino]benzonitrile
   Show/Hide
C14H9N5O3
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0545146
4-methyl-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C20H15N5
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0546886
4-fluoro-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C19H12FN5
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0546889
4-methoxy-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C20H15N5O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0550121
4-[methyl-(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzene-1,3-dicarbonitrile
   Show/Hide
C21H14N6
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0550122
4-[(3-pyridin-4-yl-1H-indazol-5-yl)oxy]benzene-1,3-dicarbonitrile
   Show/Hide
C20H11N5O
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0564489
3-nitro-4-[(2-oxo-3-pyridin-4-yl-1H-benzimidazol-5-yl)amino]benzonitrile
   Show/Hide
C19H12N6O3
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0571222
3-nitro-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C19H12N6O2
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
EC50 = 100000 nM
   TI
   LI
   LO
   TS
CP0577653
3-chloro-4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C19H12ClN5
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0339215
[4-[[4-(cyclopropylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-5-methoxyphenyl]-morpholin-4-ylmethanone
   Show/Hide
C20H21F4N5O3
 1
1
IC50 = 4 nM
   TI
   LI
   LO
   TS
CP0179674
[2-chloro-5-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C18H19ClF3N5O3
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0170077
[3-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C18H20F3N5O3
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0179673
[4-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-5-methoxyphenyl]-morpholin-4-ylmethanone
   Show/Hide
C19H21F4N5O3
 1
1
IC50 = 9 nM
   TI
   LI
   LO
   TS
CP0301154
4-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-N-(2-hydroxy-2-methylpropyl)-5-methoxybenzamide
   Show/Hide
C19H23F4N5O3
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0087578
[5-methoxy-2-methyl-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C19H22F3N5O3
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0262172
[4-[[5-bromo-4-(methylamino)pyrimidin-2-yl]amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
   Show/Hide
C17H20BrN5O3
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0349201
[2-fluoro-5-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C18H19F4N5O3
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0301155
[5-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-4-methoxypyridin-2-yl]-morpholin-4-ylmethanone
   Show/Hide
C18H21F3N6O3
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0089100
US9499542, 14
   Show/Hide
C19H16N6
 2
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
2
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0058925
2-fluoro-3-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
   Show/Hide
C17H14FN5O
 1
1
IC50 = 20 nM
   TI
   LI
   LO
   TS
CP0491719
[2,5-dimethoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C19H22F3N5O4
 1
1
IC50 = 21 nM
   TI
   LI
   LO
   TS
CP0179672
5-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-(2-hydroxy-2-methylpropyl)-6-methoxy-3H-isoindol-1-one
   Show/Hide
C20H24F3N5O3
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0301156
[5-chloro-2-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C18H19ClF3N5O3
 1
1
IC50 = 24 nM
   TI
   LI
   LO
   TS
CP0088382
3-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
   Show/Hide
C17H15N5O
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0086179
[5-chloro-4-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-methoxyphenyl]-morpholin-4-ylmethanone
   Show/Hide
C19H21ClF3N5O3
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0087577
2-N-(5-fluoro-2-methoxy-4-methylsulfonylphenyl)-4-N-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
   Show/Hide
C14H14F4N4O3S
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0155868
BDBM50396041
   Show/Hide
C17H20ClN5O3
 1
1
IC50 = 29 nM
   TI
   LI
   LO
   TS
CP0339216
[2-fluoro-3-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C18H19F4N5O3
 1
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
CP0239078
[5-chloro-2-methyl-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C18H19ClF3N5O2
 1
1
IC50 = 43 nM
   TI
   LI
   LO
   TS
CP0335187
2-N-[4-methoxy-6-(oxan-4-yl)pyridin-3-yl]-4-N-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
   Show/Hide
C17H20F3N5O2
 1
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
CP0573473
4-amino-7-methyl-2-[[5-methyl-1-[(3S)-oxolan-3-yl]pyrazol-4-yl]amino]-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H27N9O
 2
1
IC50 = 51 nM
   TI
   LI
   LO
   TS
2
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0301157
[4-[(5-bromo-4-methoxypyrimidin-2-yl)amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
   Show/Hide
C17H19BrN4O4
 1
1
IC50 = 53 nM
   TI
   LI
   LO
   TS
CP0260860
4-amino-2-[(3-chloro-1-methylpyrazol-4-yl)amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C17H20ClN9
 2
1
IC50 = 54 nM
   TI
   LI
   LO
   TS
2
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0267368
[5-fluoro-2-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C18H19F4N5O3
 1
1
IC50 = 63 nM
   TI
   LI
   LO
   TS
CP0179678
[4-[(5-chloro-4-methoxypyrimidin-2-yl)amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
   Show/Hide
C17H19ClN4O4
 1
1
IC50 = 69 nM
   TI
   LI
   LO
   TS
CP0359719
US9499542, 22
   Show/Hide
C18H15N7
 2
1
IC50 = 70 nM
   TI
   LI
   LO
   TS
2
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0482714
6-[(1-methylpyrazol-3-yl)amino]-4-(6-methylpyridin-2-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile
   Show/Hide
C18H15N7
 2
1
IC50 = 76 nM
   TI
   LI
   LO
   TS
2
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0576299
4-amino-7-methyl-2-[[5-methyl-1-[(3R)-oxolan-3-yl]pyrazol-4-yl]amino]-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H27N9O
 2
1
IC50 = 80 nM
   TI
   LI
   LO
   TS
2
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0260609
US9499542, 13
   Show/Hide
C18H14N6
 2
1
IC50 = 85 nM
   TI
   LI
   LO
   TS
2
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0085677
3-[4-(dimethylamino)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C15H13N5
 1
1
IC50 = 89 nM
   TI
   LI
   LO
   TS
CP0475020
6-[(4-chloro-1-methylpyrazol-3-yl)amino]-4-(5-methylpyridin-3-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile
   Show/Hide
C18H14ClN7
 2
1
IC50 = 93 nM
   TI
   LI
   LO
   TS
2
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0417713
6-[(4-chloro-1-methylpyrazol-3-yl)amino]-4-(6-methylpyridin-2-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile
   Show/Hide
C18H14ClN7
 2
1
IC50 = 94 nM
   TI
   LI
   LO
   TS
2
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0061269
2-N-[2-chloro-4-(1-methyltetrazol-5-yl)phenyl]-4-N-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
   Show/Hide
C14H12ClF3N8
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0169665
2-[2-methoxy-4-(morpholine-4-carbonyl)anilino]-4-(methylamino)pyrimidine-5-carbonitrile
   Show/Hide
C18H20N6O3
 1
1
IC50 = 105 nM
   TI
   LI
   LO
   TS
CP0334596
3-[4-[2-(cyanomethyl)morpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C19H16N6O
 1
1
IC50 = 117 nM
   TI
   LI
   LO
   TS
CP0260867
4-amino-2-[(1,3-dimethylpyrazol-4-yl)amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C18H23N9
 2
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
2
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0355745
4-amino-2-[[1-(2-hydroxy-2-methylpropyl)-5-methylpyrazol-4-yl]amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H29N9O
 2
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
2
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0495255
4-amino-2-[[1-[(3-hydroxyoxetan-3-yl)methyl]-5-methylpyrazol-4-yl]amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H27N9O2
 2
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
2
IC50 = 220 nM
   TI
   LI
   LO
   TS
CP0058932
3-[4-[(2S)-2-methylmorpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C18H17N5O
 1
1
IC50 = 122 nM
   TI
   LI
   LO
   TS
CP0189934
US9499542, 20
   Show/Hide
C19H17N7
 2
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
2
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0475019
6-[(1-methylpyrazol-3-yl)amino]-4-(2-methylpyridin-4-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile
   Show/Hide
C18H15N7
 2
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
2
IC50 = 700 nM
   TI
   LI
   LO
   TS
CP0085678
3-[4-[(2S)-2-(5-methyl-1,2,4-oxadiazol-3-yl)morpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C20H17N7O2
 1
1
IC50 = 133 nM
   TI
   LI
   LO
   TS
CP0575556
4-amino-7-methyl-2-[[3-methyl-1-(oxetan-3-yl)pyrazol-4-yl]amino]-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C20H25N9O
 2
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
2
IC50 = 240 nM
   TI
   LI
   LO
   TS
CP0090031
4-[5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
   Show/Hide
C16H15ClN4O
 1
1
IC50 = 144 nM
   TI
   LI
   LO
   TS
CP0461834
6-[(1,4-dimethylpyrazol-3-yl)amino]-4-(5-methylpyridin-3-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile
   Show/Hide
C19H17N7
 2
1
IC50 = 160 nM
   TI
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2
IC50 = 170 nM
   TI
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CP0575874
4-amino-2-[[1-(2-hydroxy-2-methylpropyl)-3-methylpyrazol-4-yl]amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H29N9O
 2
1
IC50 = 180 nM
   TI
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   TS
2
IC50 = 280 nM
   TI
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   TS
CP0069322
3-(4-piperidin-1-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
   Show/Hide
C18H17N5
 1
1
IC50 = 182 nM
   TI
   LI
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   TS
CP0344358
4-amino-7-methyl-2-[[5-methyl-1-(oxetan-3-yl)pyrazol-4-yl]amino]-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C20H25N9O
 2
1
IC50 = 190 nM
   TI
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2
IC50 = 300 nM
   TI
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CP0283525
4-(5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)morpholine
   Show/Hide
C16H16N4O
 1
1
IC50 = 198 nM
   TI
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CP0114275
3-[4-[(3S)-3-methylpiperidin-1-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C19H19N5
 1
1
IC50 = 210 nM
   TI
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CP0260591
US9499542, 23
   Show/Hide
C19H17N7
 2
1
IC50 = 210 nM
   TI
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2
IC50 = 580 nM
   TI
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CP0417634
6-[(4-chloro-1-methylpyrazol-3-yl)amino]-4-(2-methylpyridin-4-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonitrile
   Show/Hide
C18H14ClN7
 2
1
IC50 = 210 nM
   TI
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2
IC50 = 1300 nM
   TI
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CP0116372
4-[5-(5-methylpyridin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
   Show/Hide
C16H17N5O
 1
1
IC50 = 211 nM
   TI
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   TS
CP0334641
6-(5-chloro-2-methoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C16H13ClN6OS
 1
1
IC50 = 245 nM
   TI
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   TS
CP0573477
4-amino-2-[[1-[(3-hydroxyoxetan-3-yl)methyl]-3-methylpyrazol-4-yl]amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H27N9O2
 2
1
IC50 = 250 nM
   TI
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2
IC50 = 410 nM
   TI
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CP0578015
4-amino-2-[(1,5-dimethylpyrazol-4-yl)amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C18H23N9
 2
1
IC50 = 260 nM
   TI
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2
IC50 = 310 nM
   TI
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   TS
CP0090033
4-[5-(1-methylpyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
   Show/Hide
C14H16N6O
 1
1
IC50 = 278 nM
   TI
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   TS
CP0069326
6-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)pyridine-2-carbonitrile
   Show/Hide
C16H14N6O
 1
1
IC50 = 298 nM
   TI
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   TS
CP0069325
3-[4-[(2R)-2-methylmorpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C18H17N5O
 1
1
IC50 = 377 nM
   TI
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   LO
   TS
CP0052255
6-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C17H16N6O2S
 1
1
IC50 = 387 nM
   TI
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   TS
CP0069330
3-[4-[2-(3-methyl-1,2,4-oxadiazol-5-yl)morpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C20H17N7O2
 1
1
IC50 = 390 nM
   TI
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   TS
CP0052244
6-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazine
   Show/Hide
C18H17N5O2S
 1
1
IC50 = 400 nM
   TI
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   TS
CP0087686
[4-[[5-fluoro-4-(methylamino)pyrimidin-2-yl]amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
   Show/Hide
C17H20FN5O3
 1
1
IC50 = 418 nM
   TI
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   TS
CP0090032
3-(4-pyrrolidin-1-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
   Show/Hide
C17H15N5
 1
1
IC50 = 432 nM
   TI
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   TS
CP0480455
6-(2,5-dimethoxyphenyl)sulfanyl-3-(5-methoxypyridin-3-yl)-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C19H17N5O3S
 1
1
IC50 = 440 nM
   TI
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CP0069328
3-[4-(diethylamino)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C17H17N5
 1
1
IC50 = 443 nM
   TI
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   TS
CP0344357
4-amino-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]-2-[[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]amino]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C18H20F3N9
 2
1
IC50 = 460 nM
   TI
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2
IC50 = 910 nM
   TI
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CP0052243
5-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)pyrazolo[1,5-a]pyrimidine
   Show/Hide
C18H17N5O2S
 1
1
IC50 = 488 nM
   TI
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   TS
CP0379031
5-[6-(2,5-dimethoxyphenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
   Show/Hide
C16H13N5O2S2
 1
1
IC50 = 660 nM
   TI
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CP0143156
5-[6-(3-bromophenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
   Show/Hide
C14H8BrN5S2
 1
1
IC50 = 683 nM
   TI
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CP0302713
3-[6-(2,5-dimethoxyphenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,2-thiazole
   Show/Hide
C16H13N5O2S2
 1
1
IC50 = 722 nM
   TI
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CP0245491
6-(2,5-dimethoxyphenyl)sulfanyl-3-pyridin-3-yl-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C18H15N5O2S
 1
1
IC50 = 736 nM
   TI
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CP0052242
5-(2,5-dimethoxyphenyl)sulfanyl-2-methyl-3-(1-methylpyrazol-4-yl)pyrazolo[1,5-a]pyrimidine
   Show/Hide
C19H19N5O2S
 1
1
IC50 = 759 nM
   TI
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CP0323240
5-[6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
   Show/Hide
C15H8F3N5S2
 1
1
IC50 = 780 nM
   TI
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CP0069327
4-[5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
   Show/Hide
C17H18N4O2
 1
1
IC50 = 882 nM
   TI
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CP0419192
6-(2,5-dimethoxyphenyl)sulfanyl-2-methyl-3-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazine
   Show/Hide
C19H19N5O2S
 1
1
IC50 = 945 nM
   TI
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CP0231675
3-(1H-pyrazol-5-yl)-6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C15H9F3N6S
 1
1
IC50 = 1016 nM
   TI
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CP0322344
6-(2,5-dimethoxyphenyl)sulfanyl-3-(1,3-dimethylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C18H18N6O2S
 1
1
IC50 = 1260 nM
   TI
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CP0131134
6-(2,5-dimethoxyphenyl)sulfanyl-3-pyridin-2-yl-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C18H15N5O2S
 1
1
IC50 = 1310 nM
   TI
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CP0090034
4-[5-(3-cyanophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine-2-carbonitrile
   Show/Hide
C18H14N6O
 1
1
IC50 = 1331 nM
   TI
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CP0064440
6-(2,5-dimethoxyphenyl)sulfanyl-3-phenyl-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C19H16N4O2S
 1
1
IC50 = 1380 nM
   TI
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   TS
CP0231666
5-[6-(3-tert-butylphenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
   Show/Hide
C18H17N5S2
 1
1
IC50 = 1393 nM
   TI
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CP0231673
5-[6-(3-chlorophenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
   Show/Hide
C14H8ClN5S2
 1
1
IC50 = 1397 nM
   TI
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CP0280003
3-[4-[2-(1,2-oxazol-5-yl)morpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C20H16N6O2
 1
1
IC50 = 1467 nM
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CP0069329
3-[4-[(3R)-3-methylpiperidin-1-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C19H19N5
 1
1
IC50 = 1579 nM
   TI
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CP0174414
3-thiophen-2-yl-6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C16H9F3N4S2
 1
1
IC50 = 1656 nM
   TI
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CP0184836
2-[6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
   Show/Hide
C15H8F3N5S2
 1
1
IC50 = 1727 nM
   TI
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CP0334639
6-(2,5-dimethoxyphenoxy)-3-phenyl-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C19H16N4O3
 1
1
IC50 = 1740 nM
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CP0489450
6-(2,5-dichlorophenyl)sulfanyl-3-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C15H10Cl2N6S
 1
1
IC50 = 1800 nM
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CP0052246
4-methoxy-3-[[3-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]sulfanyl]benzonitrile
   Show/Hide
C17H13N7OS
 1
1
IC50 = 2070 nM
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CP0310490
3-fluoro-5-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
   Show/Hide
C17H14FN5O
 1
1
IC50 = 2082 nM
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CP0184815
4-[6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
   Show/Hide
C15H8F3N5S2
 1
1
IC50 = 2112 nM
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CP0317166
2-fluoro-5-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
   Show/Hide
C17H14FN5O
 1
1
IC50 = 2460 nM
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CP0085676
4-[5-(1-methylpyrazol-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
   Show/Hide
C14H16N6O
 1
1
IC50 = 2570 nM
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CP0248426
6-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-3-yl)-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C17H16N6O2S
 1
1
IC50 = 2760 nM
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CP0174408
2-[(3-thiophen-2-yl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)sulfanyl]propanamide
   Show/Hide
C12H11N5OS2
 1
1
IC50 = 3032 nM
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CP0090035
3-[4-(1,3,3a,4,6,6a-hexahydrofuro[3,4-c]pyrrol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C19H17N5O
 1
1
IC50 = 3363 nM
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CP0069323
3-[4-(2,3,3a,4,6,6a-hexahydrofuro[2,3-c]pyrrol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C19H17N5O
 1
1
IC50 = 3694 nM
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CP0476051
3-[6-(2,5-dimethoxyphenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,2-oxazole
   Show/Hide
C16H13N5O3S
 1
1
IC50 = 4330 nM
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CP0131136
5-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyridine
   Show/Hide
C17H16N6O2S
 1
1
IC50 = 5240 nM
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CP0237765
5-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)imidazo[4,5-b]pyridine
   Show/Hide
C18H17N5O2S
 1
1
IC50 = 5850 nM
   TI
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CP0085675
3-[4-(azetidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C16H13N5
 1
1
IC50 = 7687 nM
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CP0169053
4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
   Show/Hide
C17H17BrF3N7O2S
 1
1
IC50 > 10000 nM
   TI
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CP0275674
5-cyclopropyl-4-N-[2-(1H-imidazol-5-yl)ethyl]-2-N-[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]pyrimidine-2,4-diamine
   Show/Hide
C18H21F3N8
 1
1
IC50 > 10000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0644312
cis-2,6-Dimethyl-4-(6-(5-(1-methylcyclopropoxy)-1H-indazol-3-yl)pyrimidin-4-yl)morpholine
   Show/Hide
C21H25N5O2
 8
1 EC50 ~ 1.22 nM
2 IC50 = 0.4 nM
3 IC50 = 0.5 nM
4 IC50 = 0.76 nM
5 IC50 = 1 nM
6 IC50 ~ 1.8 nM
7 IC50 ~ 3.5 nM
8 IC50 ~ 6.3 nM
CP0141818
[3-(difluoromethoxy)-4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]-(4-methylpiperazin-1-yl)methanone
   Show/Hide
C21H24F2N6O3
 1
1 IC50 < 0.1585 nM
CP0019734
4-(propan-2-ylamino)-6-(1H-pyrazol-4-yl)cinnoline-3-carboxamide
   Show/Hide
C15H16N6O
 2
1 IC50 = 1 nM
2 IC50 = 5 nM
CP0023856
4-[[(1R)-1-cyclopropylethyl]amino]-7-(4-methylsulfonylphenyl)cinnoline-3-carboxamide
   Show/Hide
C21H22N4O3S
 2
1 IC50 = 1 nM
2 IC50 = 7 nM
CP0067767
4-[[(2R)-butan-2-yl]amino]-7-(4-methylsulfonylphenyl)cinnoline-3-carboxamide
   Show/Hide
C20H22N4O3S
 2
1 IC50 = 1 nM
2 IC50 = 4 nM
CP0357679
N-[2-[(3R)-3-(2-hydroxypropan-2-yl)pyrrolidin-1-yl]-5-(trifluoromethyl)pyridin-4-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
   Show/Hide
C23H25F3N6O2
 1
1 IC50 = 1 nM
CP0033205
(5R)-5-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
   Show/Hide
C24H21N5
 2
1 IC50 < 1 nM
2 IC50 = 14 nM
CP0033544
2-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]benzonitrile
   Show/Hide
C20H15N5
 2
1 IC50 = 1 nM
2 IC50 = 5 nM
CP0546499
(5S)-5-[[3-(2,6-dimethylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
   Show/Hide
C25H23N5
 2
1 IC50 < 1 nM
2 IC50 = 11 nM
CP0564501
(5S)-5-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
   Show/Hide
C24H21N5
 2
1 IC50 < 1 nM
2 IC50 = 8 nM
CP0572904
(5S)-5-[[3-(2-morpholin-4-ylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
   Show/Hide
C27H26N6O
 2
1 IC50 < 1 nM
2 IC50 = 8 nM
CP0218399
4-[[(1R)-1-cyclopropylethyl]amino]-7-pyridin-4-ylcinnoline-3-carboxamide
   Show/Hide
C19H19N5O
 3
1 IC50 = 2 nM
2 IC50 = 6 nM
3 IC50 <= 6 nM
CP0535015
N-[2-[(2R,3S)-3-hydroxy-2-methylazetidin-1-yl]-5-(trifluoromethyl)pyridin-4-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
   Show/Hide
C20H19F3N6O2
 1
1 IC50 = 2 nM
CP0564492
3-fluoro-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C19H12FN5
 2
1 IC50 = 2 nM
2 IC50 = 10 nM
CP0568003
4-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]benzene-1,3-dicarbonitrile
   Show/Hide
C21H14N6
 2
1 IC50 = 2 nM
2 IC50 = 7 nM
CP0579368
(5R)-5-[[3-(2-morpholin-4-ylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C27H26N6O
 2
1 IC50 = 2 nM
2 IC50 = 30 nM
CP0058925
2-fluoro-3-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
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C17H14FN5O
 2
1 IC50 = 3 nM
2 IC50 = 9 nM
CP0088382
3-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
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C17H15N5O
 3
1 IC50 = 3 nM
2 IC50 = 11 nM
3 IC50 = 15 nM
CP0570264
(5S)-5-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C23H19N5
 2
1 IC50 = 3 nM
2 IC50 = 40 nM
CP0577522
2-[[3-(2-methoxypyridin-4-yl)-1H-indazol-5-yl]amino]benzonitrile
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C20H15N5O
 2
1 IC50 = 3 nM
2 IC50 = 21 nM
CP0899198
(S)-(4-((4-Ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl)methanone
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C23H28N6O3
 1
1 IC50 = 3.162 nM
CP0083561
BDBM50379529
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C31H38N8O3
 4
1 IC50 = 3.5 nM
2 IC50 = 6 nM
3 IC50 = 13 nM
4 Ki = 6 nM
CP0357657
N-[2-[(2S,6R)-2,6-dimethylmorpholin-4-yl]-5-(trifluoromethyl)pyridin-4-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
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C22H23F3N6O2
 1
1 IC50 = 4 nM
CP0571039
N-[6-[(3R)-3-(2-hydroxypropan-2-yl)pyrrolidin-1-yl]-2-methylpyrimidin-4-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
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C22H27N7O2
 1
1 IC50 = 4 nM
CP0543315
(4R)-4-[[3-(2,6-dimethylpyridin-4-yl)-1H-indazol-5-yl]amino]-3,4-dihydro-2H-chromene-7-carbonitrile
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C24H21N5O
 2
1 IC50 = 4 nM
2 IC50 = 42 nM
CP0564488
4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-3,4-dihydro-2H-chromene-7-carbonitrile
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C22H17N5O
 2
1 IC50 = 4 nM
2 IC50 = 61 nM
CP0568096
N-(2-nitrophenyl)-3-pyridin-4-yl-1H-indazol-5-amine
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C18H13N5O2
 2
1 IC50 = 4 nM
2 IC50 = 24 nM
CP0568097
2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H13N5
 2
1 IC50 = 4 nM
2 IC50 = 19 nM
CP0568785
(5R)-5-[[3-(2,6-dimethylpyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C25H23N5
 2
1 IC50 = 4 nM
2 IC50 = 35 nM
CP0535014
N-[2-(3-hydroxyazetidin-1-yl)-5-(trifluoromethyl)pyridin-4-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
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C19H17F3N6O2
 1
1 IC50 = 4.8 nM
CP0019820
7-(1-methylpyrazol-4-yl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
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C17H17N5
 2
1 IC50 = 5 nM
2 IC50 = 7 nM
CP0085677
3-[4-(dimethylamino)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
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C15H13N5
 3
1 IC50 = 5 nM
2 IC50 = 15 nM
3 IC50 = 42 nM
CP0334596
3-[4-[2-(cyanomethyl)morpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
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C19H16N6O
 1
1 IC50 = 5 nM
CP0575973
N-[2-[(2R,3R)-3-hydroxy-2-methylpyrrolidin-1-yl]-5-(trifluoromethyl)pyridin-4-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
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C21H21F3N6O2
 1
1 IC50 = 5 nM
CP0572902
2-fluoro-6-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H12FN5
 2
1 IC50 = 5 nM
2 IC50 = 22 nM
CP0574429
1-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-2,3-dihydro-1H-indene-5-carbonitrile
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C22H17N5
 2
1 IC50 = 5 nM
2 IC50 = 40 nM
CP0321712
4-[3-cyano-4-(propan-2-ylamino)quinolin-7-yl]-N-methylbenzenesulfonamide
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C20H20N4O2S
 2
1 IC50 = 6 nM
2 IC50 = 9 nM
CP0143156
5-[6-(3-bromophenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
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C14H8BrN5S2
 2
1 IC50 = 6 nM
2 IC50 = 32 nM
CP0069322
3-(4-piperidin-1-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
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C18H17N5
 2
1 IC50 = 6 nM
2 IC50 = 28 nM
CP0094235
5-(4-methylpiperazin-1-yl)-2-phenylmethoxy-N-pyridin-3-ylbenzamide
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C24H26N4O2
 1
1 IC50 = 6 nM
CP0031119
4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzene-1,3-dicarbonitrile
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C20H12N6
 2
1 IC50 = 6 nM
2 IC50 = 34 nM
CP0545147
5-methyl-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C20H15N5
 2
1 IC50 = 6 nM
2 IC50 = 18 nM
CP0031120
3-nitro-4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H12N6O2
 2
1 IC50 = 6.2 nM
2 IC50 = 23 nM
CP0322693
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]-3-methoxyphenyl]-(2-methyl-2,7-diazaspiro[3.5]nonan-7-yl)methanone
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C24H30N6O3
 1
1 IC50 = 6.31 nM
CP0537119
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]-3-methoxyphenyl]-(4-fluoropiperidin-1-yl)methanone
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C21H24FN5O3
 1
1 IC50 = 6.31 nM
CP0058932
3-[4-[(2S)-2-methylmorpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
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C18H17N5O
 1
1 IC50 = 7 nM
CP0546878
5-methoxy-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C20H15N5O
 2
1 IC50 = 7 nM
2 IC50 = 22 nM
CP0072337
2-[(4-fluorophenyl)methoxy]-N-pyridin-3-yl-5-(trifluoromethyl)benzamide
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C20H14F4N2O2
 2
1 IC50 = 7.943 nM
2 IC50 = 19.95 nM
CP0353350
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]-morpholin-4-ylmethanone
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C19H21N5O3
 1
1 IC50 = 7.943 nM
CP0807578
(S)-(4-((4-Ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(3-methylmorpholino)methanone
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C21H25N5O4
 1
1 IC50 = 7.943 nM
CP0838494
(R)-(4-((4-Ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl)methanone
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C23H28N6O3
 1
1 IC50 = 7.943 nM
CP0231673
5-[6-(3-chlorophenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
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C14H8ClN5S2
 2
1 IC50 = 8 nM
2 IC50 = 31 nM
CP0085678
3-[4-[(2S)-2-(5-methyl-1,2,4-oxadiazol-3-yl)morpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
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C20H17N7O2
 1
1 IC50 = 8 nM
CP0090031
4-[5-(3-chlorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
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C16H15ClN4O
 2
1 IC50 = 8 nM
2 IC50 = 13 nM
CP0090032
3-(4-pyrrolidin-1-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
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C17H15N5
 2
1 IC50 = 8 nM
2 IC50 = 64 nM
CP0577559
N-[5-[(3R)-3-(2-hydroxypropan-2-yl)pyrrolidin-1-yl]-2-(trifluoromethyl)pyridin-3-yl]-6-[1-[[1-(trifluoromethyl)cyclopropyl]methyl]pyrazol-4-yl]pyridine-2-carboxamide
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C27H28F6N6O2
 1
1 IC50 = 8 nM
CP0564486
3-methyl-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C20H15N5
 2
1 IC50 = 8 nM
2 IC50 = 25 nM
CP0564491
2-[(3-pyridin-4-yl-1H-indazol-5-yl)oxy]benzonitrile
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C19H12N4O
 2
1 IC50 = 8 nM
2 IC50 = 20 nM
CP0573657
(4R)-4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-3,4-dihydro-2H-chromene-7-carbonitrile
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C22H17N5O
 2
1 IC50 = 8 nM
2 IC50 = 189 nM
CP0573659
2-methyl-6-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C20H15N5
 2
1 IC50 = 8 nM
2 IC50 = 38 nM
CP0357660
6-[1-(cyclopropylmethyl)pyrazol-4-yl]-N-[5-[(3R)-3-(2-hydroxypropan-2-yl)pyrrolidin-1-yl]-2-(trifluoromethyl)pyridin-3-yl]pyridine-2-carboxamide
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C26H29F3N6O2
 1
1 IC50 = 8.6 nM
CP0069326
6-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)pyridine-2-carbonitrile
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C16H14N6O
 2
1 IC50 = 9 nM
2 IC50 = 26 nM
CP0283525
4-(5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)morpholine
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C16H16N4O
 2
1 IC50 = 9 nM
2 IC50 = 14 nM
CP0357658
N-[2-[4-(2-hydroxypropan-2-yl)-2-azabicyclo[2.1.1]hexan-2-yl]-5-(trifluoromethyl)pyridin-4-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
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C24H25F3N6O2
 1
1 IC50 = 9 nM
CP0535011
N-[2-[(2S,6R)-2,6-dimethylmorpholin-4-yl]-5-methylpyridin-4-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
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C22H26N6O2
 1
1 IC50 = 9 nM
CP0543316
(5R)-5-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C23H19N5
 2
1 IC50 = 9 nM
2 IC50 = 115 nM
CP0077182
7-(4-morpholin-4-ylsulfonylphenyl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
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C23H24N4O3S
 2
1 IC50 = 10 nM
2 IC50 = 14 nM
CP0114881
4-(azetidin-1-yl)-7-(1-methylpyrazol-4-yl)quinoline-3-carbonitrile
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C17H15N5
 2
1 IC50 = 10 nM
2 IC50 = 13 nM
CP0507459
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]-3-propan-2-yloxyphenyl]-(4-methylpiperazin-1-yl)methanone
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C23H30N6O3
 1
1 IC50 = 10 nM
CP0507460
[3-ethoxy-4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]-(4-methylpiperazin-1-yl)methanone
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C22H28N6O3
 1
1 IC50 = 10 nM
CP0549589
[3-ethoxy-4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]-morpholin-4-ylmethanone
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C21H25N5O4
 1
1 IC50 = 10 nM
CP0495255
4-amino-2-[[1-[(3-hydroxyoxetan-3-yl)methyl]-5-methylpyrazol-4-yl]amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
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C21H27N9O2
 2
1 IC50 = 10 nM
2 IC50 = 16 nM
CP0571036
N-[5-[(3R)-3-(2-hydroxypropan-2-yl)pyrrolidin-1-yl]-2-(trifluoromethyl)pyridin-3-yl]-6-[1-(2,2,2-trifluoroethyl)pyrazol-4-yl]pyridine-2-carboxamide
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C24H24F6N6O2
 1
1 IC50 = 10 nM
CP0577652
3-nitro-4-[(3-pyridin-4-yl-1H-indazol-5-yl)oxy]benzonitrile
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C19H11N5O3
 2
1 IC50 = 10 nM
2 IC50 = 26 nM
CP0546879
2-methyl-3-[[(3-pyridin-4-yl-1H-indazol-5-yl)amino]methyl]benzonitrile
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C21H17N5
 2
1 IC50 = 11 nM
2 IC50 = 82 nM
CP0090033
4-[5-(1-methylpyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
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C14H16N6O
 3
1 IC50 = 12 nM
2 IC50 = 36 nM
3 IC50 = 50 nM
CP0576299
4-amino-7-methyl-2-[[5-methyl-1-[(3R)-oxolan-3-yl]pyrazol-4-yl]amino]-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H27N9O
 2
1 IC50 = 12 nM
2 IC50 = 20 nM
CP0550091
(5R)-5-[[3-(1-methylpyrazol-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C22H20N6
 2
1 IC50 = 12 nM
2 IC50 = 69 nM
CP0031357
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
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C20H23N5O4
 1
1 IC50 = 12.59 nM
CP0425397
4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]-N-(2-hydroxy-2-methylpropyl)-3-methoxybenzamide
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C20H25N5O4
 1
1 IC50 = 12.59 nM
CP0517316
[3-chloro-4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]-(4-methylpiperazin-1-yl)methanone
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C20H23ClN6O2
 1
1 IC50 = 12.59 nM
CP0532672
4-[[4-(2,2,2-trifluoroethylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]benzamide
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C15H13F3N6O
 1
1 IC50 = 12.59 nM
CP0553334
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]-3-fluorophenyl]-(4-methylpiperazin-1-yl)methanone
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C20H23FN6O2
 1
1 IC50 = 12.59 nM
CP0557934
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]-(4-methylpiperazin-1-yl)methanone
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C20H24N6O2
 1
1 IC50 = 12.59 nM
CP0561897
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]-3-propan-2-yloxyphenyl]-morpholin-4-ylmethanone
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C22H27N5O4
 1
1 IC50 = 12.59 nM
CP0231675
3-(1H-pyrazol-5-yl)-6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazine
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C15H9F3N6S
 2
1 IC50 = 13 nM
2 IC50 = 53 nM
CP0543313
5-fluoro-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H12FN5
 2
1 IC50 = 13 nM
2 IC50 = 56 nM
CP0233613
4-(propan-2-ylamino)-7-(1,2-thiazol-4-yl)cinnoline-3-carboxamide
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C15H15N5OS
 2
1 IC50 = 14 nM
2 IC50 = 20 nM
CP0573473
4-amino-7-methyl-2-[[5-methyl-1-[(3S)-oxolan-3-yl]pyrazol-4-yl]amino]-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H27N9O
 2
1 IC50 = 14 nM
2 IC50 = 23 nM
CP0573705
N-(1-cyclobutylpyrazol-4-yl)-2-(1-methylpyrazol-4-yl)-1,3-thiazole-4-carboxamide
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C15H16N6OS
 1
1 IC50 = 14 nM
CP0022216
4-(propan-2-ylamino)-7-pyridin-4-ylcinnoline-3-carboxamide
   Show/Hide
C17H17N5O
 2
1 IC50 = 15 nM
2 IC50 = 16 nM
CP0067768
7-(4-methylsulfonylphenyl)-4-(propan-2-ylamino)cinnoline-3-carboxamide
   Show/Hide
C19H20N4O3S
 2
1 IC50 = 15 nM
2 IC50 = 27 nM
CP0549590
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]-3-methoxyphenyl]-(4-methylpiperazin-1-yl)methanone
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C21H26N6O3
 1
1 IC50 = 15.85 nM
CP0838495
(R)-(4-((4-Ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)(3-methylmorpholino)methanone
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C21H25N5O4
 1
1 IC50 = 15.85 nM
CP0185411
7-(2-methyl-1,3-thiazol-5-yl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
   Show/Hide
C17H16N4S
 2
1 IC50 = 16 nM
2 IC50 = 23 nM
CP0114275
3-[4-[(3S)-3-methylpiperidin-1-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C19H19N5
 2
1 IC50 = 16 nM
2 IC50 = 49 nM
CP0578424
4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C19H13N5
 2
1 IC50 = 16 nM
2 IC50 = 57 nM
CP0554356
N-[5-[(3R)-3-(2-hydroxypropan-2-yl)pyrrolidin-1-yl]-2-(trifluoromethyl)pyridin-3-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
   Show/Hide
C23H25F3N6O2
 1
1 IC50 = 17 nM
CP0568101
(5R)-5-[(6-fluoro-3-pyridin-4-yl-1H-indazol-5-yl)amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
   Show/Hide
C23H18FN5
 2
1 IC50 = 17 nM
2 IC50 = 218 nM
CP0323240
5-[6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
   Show/Hide
C15H8F3N5S2
 2
1 IC50 = 18 nM
2 IC50 = 74 nM
CP0069325
3-[4-[(2R)-2-methylmorpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C18H17N5O
 1
1 IC50 = 18 nM
CP0116372
4-[5-(5-methylpyridin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
   Show/Hide
C16H17N5O
 2
1 IC50 = 18 nM
2 IC50 = 30 nM
CP0562897
6-(1-cyclobutylpyrazol-4-yl)-N-[5-[(3R)-3-(2-hydroxypropan-2-yl)pyrrolidin-1-yl]-2-(trifluoromethyl)pyridin-3-yl]pyridine-2-carboxamide
   Show/Hide
C26H29F3N6O2
 1
1 IC50 = 19 nM
CP0065744
4-(dimethylamino)-7-(4-methylsulfonylphenyl)quinoline-3-carbonitrile
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C19H17N3O2S
 2
1 IC50 = 20 nM
2 IC50 = 27 nM
CP0069328
3-[4-(diethylamino)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
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C17H17N5
 2
1 IC50 = 20 nM
2 IC50 = 151 nM
CP0069330
3-[4-[2-(3-methyl-1,2,4-oxadiazol-5-yl)morpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
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C20H17N7O2
 1
1 IC50 = 20 nM
CP0155868
BDBM50396041
   Show/Hide
C17H20ClN5O3
 2
1 IC50 = 20.3 nM
2 Ki = 3 nM
CP0260860
4-amino-2-[(3-chloro-1-methylpyrazol-4-yl)amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C17H20ClN9
 2
1 IC50 = 21 nM
2 IC50 = 34 nM
CP0568098
3-[[(3-pyridin-4-yl-1H-indazol-5-yl)amino]methyl]benzonitrile
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C20H15N5
 2
1 IC50 = 21 nM
2 IC50 = 26 nM
CP0174414
3-thiophen-2-yl-6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazine
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C16H9F3N4S2
 2
1 IC50 = 23 nM
2 IC50 = 75 nM
CP0564500
3-[(1S)-1-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]ethyl]benzonitrile
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C21H17N5
 2
1 IC50 = 23 nM
2 IC50 = 67 nM
CP0184836
2-[6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
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C15H8F3N5S2
 2
1 IC50 = 25 nM
2 IC50 = 88 nM
CP0575556
4-amino-7-methyl-2-[[3-methyl-1-(oxetan-3-yl)pyrazol-4-yl]amino]-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C20H25N9O
 2
1 IC50 = 25 nM
2 IC50 = 38 nM
CP0019480
4-[[(1R)-1-cyclopropylethyl]amino]-7-[4-(2-oxo-1,3-oxazol-3-yl)phenyl]quinoline-3-carbonitrile
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C24H20N4O2
 2
1 IC50 = 27 nM
2 IC50 = 48 nM
CP0016537
7-(4-methylsulfonylphenyl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
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C20H19N3O2S
 2
1 IC50 = 28 nM
2 IC50 = 31 nM
CP0069327
4-[5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
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C17H18N4O2
 2
1 IC50 = 28 nM
2 IC50 = 46 nM
CP0357678
N-[2-(3-methoxyazetidin-1-yl)-5-(trifluoromethyl)pyridin-4-yl]-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
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C20H19F3N6O2
 1
1 IC50 = 28 nM
CP0550119
(4R)-4-[[3-(2-methylpyridin-4-yl)-1H-indazol-5-yl]amino]-3,4-dihydro-2H-chromene-7-carbonitrile
   Show/Hide
C23H19N5O
 2
1 IC50 = 29 nM
2 IC50 = 132 nM
CP0231666
5-[6-(3-tert-butylphenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
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C18H17N5S2
 2
1 IC50 = 30 nM
2 IC50 = 75 nM
CP0260867
4-amino-2-[(1,3-dimethylpyrazol-4-yl)amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
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C18H23N9
 4
1 IC50 = 30 nM
2 IC50 = 38 nM
3 Ki = 1 nM
4 Ki = 2 nM
CP0357656
N-(1-cyclobutylpyrazol-4-yl)-2-(1-methylpyrazol-4-yl)pyrimidine-4-carboxamide
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C16H17N7O
 1
1 IC50 = 34 nM
CP0184815
4-[6-[3-(trifluoromethyl)phenyl]sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
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C15H8F3N5S2
 2
1 IC50 = 35 nM
2 IC50 = 140 nM
CP0355745
4-amino-2-[[1-(2-hydroxy-2-methylpropyl)-5-methylpyrazol-4-yl]amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H29N9O
 2
1 IC50 = 35 nM
2 IC50 = 43 nM
CP0280003
3-[4-[2-(1,2-oxazol-5-yl)morpholin-4-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
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C20H16N6O2
 1
1 IC50 = 37 nM
CP0344358
4-amino-7-methyl-2-[[5-methyl-1-(oxetan-3-yl)pyrazol-4-yl]amino]-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C20H25N9O
 2
1 IC50 = 37 nM
2 IC50 = 47 nM
CP0550122
4-[(3-pyridin-4-yl-1H-indazol-5-yl)oxy]benzene-1,3-dicarbonitrile
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C20H11N5O
 2
1 IC50 = 38 nM
2 IC50 = 48 nM
CP0064440
6-(2,5-dimethoxyphenyl)sulfanyl-3-phenyl-[1,2,4]triazolo[4,3-b]pyridazine
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C19H16N4O2S
 3
1 IC50 = 40 nM
2 IC50 = 82 nM
3 IC50 = 173 nM
CP0546302
6-(1-ethylpyrazol-4-yl)-N-[5-[(3R)-3-(2-hydroxypropan-2-yl)pyrrolidin-1-yl]-2-(trifluoromethyl)pyridin-3-yl]pyridine-2-carboxamide
   Show/Hide
C24H27F3N6O2
 1
1 IC50 = 40 nM
CP0090034
4-[5-(3-cyanophenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine-2-carbonitrile
   Show/Hide
C18H14N6O
 1
1 IC50 = 42 nM
CP0575874
4-amino-2-[[1-(2-hydroxy-2-methylpropyl)-3-methylpyrazol-4-yl]amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H29N9O
 2
1 IC50 = 42 nM
2 IC50 = 49 nM
CP0550120
N-(3,4-dihydro-2H-chromen-4-yl)-3-pyridin-4-yl-1H-indazol-5-amine
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C21H18N4O
 2
1 IC50 = 42 nM
2 IC50 = 154 nM
CP0578015
4-amino-2-[(1,5-dimethylpyrazol-4-yl)amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
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C18H23N9
 4
1 IC50 = 43 nM
2 IC50 = 75 nM
3 Ki = 2 nM
4 Ki = 3 nM
CP0550117
4-[[(3-pyridin-4-yl-1H-indazol-5-yl)amino]methyl]benzonitrile
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C20H15N5
 2
1 IC50 = 43 nM
2 IC50 = 48 nM
CP0262506
7-(6-methylsulfonylpyridin-3-yl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
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C19H18N4O2S
 2
1 IC50 = 48 nM
2 IC50 = 64 nM
CP0174408
2-[(3-thiophen-2-yl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)sulfanyl]propanamide
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C12H11N5OS2
 2
1 IC50 = 48 nM
2 IC50 = 98 nM
CP0564490
3-methyl-4-[(3-pyridin-4-yl-1H-indazol-5-yl)oxy]benzonitrile
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C20H14N4O
 2
1 IC50 = 50 nM
2 IC50 = 134 nM
CP0573477
4-amino-2-[[1-[(3-hydroxyoxetan-3-yl)methyl]-3-methylpyrazol-4-yl]amino]-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C21H27N9O2
 2
1 IC50 = 51 nM
2 IC50 = 57 nM
CP0568099
(5R)-5-[[3-(2-methoxypyridin-4-yl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
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C24H21N5O
 2
1 IC50 = 51 nM
2 IC50 = 637 nM
CP0077181
7-(4-methylsulfonylphenyl)-4-piperidin-1-ylquinoline-3-carbonitrile
   Show/Hide
C22H21N3O2S
 2
1 IC50 = 52 nM
2 IC50 = 59 nM
CP0085676
4-[5-(1-methylpyrazol-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]morpholine
   Show/Hide
C14H16N6O
 2
1 IC50 = 53 nM
2 IC50 = 90 nM
CP0535010
N-(1-cyclobutylpyrazol-4-yl)-6-(1-methylpyrazol-4-yl)pyridine-2-carboxamide
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C17H18N6O
 1
1 IC50 = 53 nM
CP0571222
3-nitro-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C19H12N6O2
 2
1 IC50 = 54 nM
2 IC50 = 118 nM
CP0573658
3-methoxy-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C20H15N5O
 2
1 IC50 = 54 nM
2 IC50 = 156 nM
CP0466116
[4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]-3-methoxyphenyl]-(2-oxa-6-azaspiro[3.3]heptan-6-yl)methanone
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C21H23N5O4
 1
1 IC50 = 63.1 nM
CP0920744
((2R,6S)-2,6-Dimethylmorpholino)(4-((4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxyphenyl)methanone
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C22H27N5O4
 1
1 IC50 = 63.1 nM
CP0052243
5-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)pyrazolo[1,5-a]pyrimidine
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C18H17N5O2S
 1
1 IC50 = 64 nM
CP0052246
4-methoxy-3-[[3-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]sulfanyl]benzonitrile
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C17H13N7OS
 1
1 IC50 = 64 nM
CP0052255
6-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazine
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C17H16N6O2S
 1
1 IC50 = 64 nM
CP0065790
7-(5-chlorothiophen-2-yl)-4-(propan-2-ylamino)quinoline-3-carbonitrile
   Show/Hide
C17H14ClN3S
 2
1 IC50 = 65 nM
2 IC50 = 109 nM
CP0480455
6-(2,5-dimethoxyphenyl)sulfanyl-3-(5-methoxypyridin-3-yl)-[1,2,4]triazolo[4,3-b]pyridazine
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C19H17N5O3S
 1
1 IC50 = 66 nM
CP0052244
6-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazine
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C18H17N5O2S
 1
1 IC50 = 69 nM
CP0069329
3-[4-[(3R)-3-methylpiperidin-1-yl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
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C19H19N5
 2
1 IC50 = 69 nM
2 IC50 = 171 nM
CP0574337
N-(1-cyclobutylpyrazol-4-yl)-2-fluoro-3-(1-methylpyrazol-4-yl)benzamide
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C18H18FN5O
 1
1 IC50 = 70 nM
CP0334641
6-(5-chloro-2-methoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazine
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C16H13ClN6OS
 1
1 IC50 = 78 nM
CP0310490
3-fluoro-5-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
   Show/Hide
C17H14FN5O
 2
1 IC50 = 80 nM
2 IC50 = 688 nM
CP0546886
4-fluoro-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H12FN5
 2
1 IC50 = 81 nM
2 IC50 = 163 nM
CP0275674
5-cyclopropyl-4-N-[2-(1H-imidazol-5-yl)ethyl]-2-N-[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]pyrimidine-2,4-diamine
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C18H21F3N8
 1
1 IC50 = 89 nM
CP0302713
3-[6-(2,5-dimethoxyphenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,2-thiazole
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C16H13N5O2S2
 1
1 IC50 = 91 nM
CP0379031
5-[6-(2,5-dimethoxyphenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,3-thiazole
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C16H13N5O2S2
 1
1 IC50 = 95 nM
CP0179673
[4-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-5-methoxyphenyl]-morpholin-4-ylmethanone
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C19H21F4N5O3
 3
1 IC50 = 97 nM
2 Ki = 1 nM
3 Ki = 2 nM
CP0158844
5-morpholin-4-yl-2-phenylmethoxy-N-pyridazin-4-ylbenzamide
   Show/Hide
C22H22N4O3
 2
1 IC50 = 100 nM
2 IC50 = 158.49 nM
CP0577653
3-chloro-4-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
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C19H12ClN5
 2
1 IC50 = 102 nM
2 IC50 = 227 nM
CP0052242
5-(2,5-dimethoxyphenyl)sulfanyl-2-methyl-3-(1-methylpyrazol-4-yl)pyrazolo[1,5-a]pyrimidine
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C19H19N5O2S
 1
1 IC50 = 110 nM
CP0419192
6-(2,5-dimethoxyphenyl)sulfanyl-2-methyl-3-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazine
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C19H19N5O2S
 1
1 IC50 = 115 nM
CP0085675
3-[4-(azetidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C16H13N5
 2
1 IC50 = 115 nM
2 IC50 = 325 nM
CP0317166
2-fluoro-5-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile
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C17H14FN5O
 2
1 IC50 = 117 nM
2 IC50 = 920 nM
CP0069323
3-[4-(2,3,3a,4,6,6a-hexahydrofuro[2,3-c]pyrrol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C19H17N5O
 1
1 IC50 = 139 nM
CP0546880
5-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]naphthalene-2-carbonitrile
   Show/Hide
C23H15N5
 2
1 IC50 = 150 nM
2 IC50 = 527 nM
CP0169053
4-[[[5-bromo-2-[[3-methyl-1-(2,2,2-trifluoroethyl)pyrazol-4-yl]amino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide
   Show/Hide
C17H17BrF3N7O2S
 1
1 IC50 = 159 nM
CP0543311
(5R)-5-[[3-pyridin-4-yl-6-(trifluoromethyl)-1H-indazol-5-yl]amino]-5,6,7,8-tetrahydronaphthalene-2-carbonitrile
   Show/Hide
C24H18F3N5
 2
1 IC50 = 163 nM
2 IC50 = 646 nM
CP0550121
4-[methyl-(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzene-1,3-dicarbonitrile
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C21H14N6
 2
1 IC50 = 163 nM
2 IC50 = 346 nM
CP0545146
4-methyl-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C20H15N5
 2
1 IC50 = 197 nM
2 IC50 = 276 nM
CP0219174
[3-(dimethylamino)-4-[(4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino]phenyl]-(4-methylpiperazin-1-yl)methanone
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C22H29N7O2
 1
1 IC50 = 199.53 nM
CP0090035
3-[4-(1,3,3a,4,6,6a-hexahydrofuro[3,4-c]pyrrol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile
   Show/Hide
C19H17N5O
 1
1 IC50 = 222 nM
CP0248426
6-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-3-yl)-[1,2,4]triazolo[4,3-b]pyridazine
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C17H16N6O2S
 1
1 IC50 = 224 nM
CP0334639
6-(2,5-dimethoxyphenoxy)-3-phenyl-[1,2,4]triazolo[4,3-b]pyridazine
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C19H16N4O3
 1
1 IC50 = 236 nM
CP0245491
6-(2,5-dimethoxyphenyl)sulfanyl-3-pyridin-3-yl-[1,2,4]triazolo[4,3-b]pyridazine
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C18H15N5O2S
 1
1 IC50 = 242 nM
CP0238014
5-[4-(2-methoxyethyl)piperazin-1-yl]-2-phenylmethoxy-N-pyridazin-4-ylbenzamide
   Show/Hide
C25H29N5O3
 2
1 IC50 = 251.19 nM
2 IC50 = 398.11 nM
CP0052034
US9321748, 12
   Show/Hide
C21H26N6O
 1
1 IC50 = 300 nM
CP0322344
6-(2,5-dimethoxyphenyl)sulfanyl-3-(1,3-dimethylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C18H18N6O2S
 1
1 IC50 = 323 nM
CP0344357
4-amino-7-methyl-6-[(2R)-2-methylpyrrolidin-1-yl]-2-[[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]amino]pyrrolo[2,3-d]pyrimidine-5-carbonitrile
   Show/Hide
C18H20F3N9
 2
1 IC50 = 358 nM
2 IC50 = 508 nM
CP0546889
4-methoxy-2-[(3-pyridin-4-yl-1H-indazol-5-yl)amino]benzonitrile
   Show/Hide
C20H15N5O
 2
1 IC50 = 371 nM
2 IC50 = 866 nM
CP0489450
6-(2,5-dichlorophenyl)sulfanyl-3-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazine
   Show/Hide
C15H10Cl2N6S
 1
1 IC50 = 373 nM
CP0152600
3-nitro-4-[(2-oxo-1,3-dihydrobenzimidazol-5-yl)amino]benzonitrile
   Show/Hide
C14H9N5O3
 4
1 IC50 = 450 nM
2 IC50 = 500 nM
3 IC50 = 3300 nM
4 IC50 = 11100 nM
CP0131134
6-(2,5-dimethoxyphenyl)sulfanyl-3-pyridin-2-yl-[1,2,4]triazolo[4,3-b]pyridazine
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C18H15N5O2S
 1
1 IC50 = 496 nM
CP0131136
5-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyridine
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C17H16N6O2S
 1
1 IC50 = 525 nM
CP0237765
5-(2,5-dimethoxyphenyl)sulfanyl-3-(1-methylpyrazol-4-yl)imidazo[4,5-b]pyridine
   Show/Hide
C18H17N5O2S
 1
1 IC50 = 661 nM
CP0476051
3-[6-(2,5-dimethoxyphenyl)sulfanyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]-1,2-oxazole
   Show/Hide
C16H13N5O3S
 1
1 IC50 = 804 nM
CP0564489
3-nitro-4-[(2-oxo-3-pyridin-4-yl-1H-benzimidazol-5-yl)amino]benzonitrile
   Show/Hide
C19H12N6O3
 2
1 IC50 = 5110 nM
2 IC50 = 10000 nM
CP0019908
BDBM50242742
   Show/Hide
C30H40ClN7O3S
 2
1 Kd = 0.86 nM
2 Kd = 1.4 nM
CP0170077
[3-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
   Show/Hide
C18H20F3N5O3
 3
1 Ki = 1 nM
2 Ki = 2 nM
3 Ki = 2.7 nM
CP0262172
[4-[[5-bromo-4-(methylamino)pyrimidin-2-yl]amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
   Show/Hide
C17H20BrN5O3
 2
1 Ki = 1 nM
2 Ki = 2 nM
CP0301154
4-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-N-(2-hydroxy-2-methylpropyl)-5-methoxybenzamide
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C19H23F4N5O3
 1
1 Ki = 1 nM
CP0339215
[4-[[4-(cyclopropylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-5-methoxyphenyl]-morpholin-4-ylmethanone
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C20H21F4N5O3
 1
1 Ki = 1 nM
CP0491719
[2,5-dimethoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
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C19H22F3N5O4
 1
1 Ki = 1 nM
CP0087577
2-N-(5-fluoro-2-methoxy-4-methylsulfonylphenyl)-4-N-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
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C14H14F4N4O3S
 2
1 Ki = 2 nM
2 Ki = 3 nM
CP0087578
[5-methoxy-2-methyl-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
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C19H22F3N5O3
 1
1 Ki = 2 nM
CP0179674
[2-chloro-5-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
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C18H19ClF3N5O3
 1
1 Ki = 2 nM
CP0301156
[5-chloro-2-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
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C18H19ClF3N5O3
 2
1 Ki = 2 nM
2 Ki = 4 nM
CP0169665
2-[2-methoxy-4-(morpholine-4-carbonyl)anilino]-4-(methylamino)pyrimidine-5-carbonitrile
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C18H20N6O3
 3
1 Ki = 2.4 nM
2 Ki = 11 nM
3 Ki = 13 nM
CP0349201
[2-fluoro-5-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
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C18H19F4N5O3
 2
1 Ki = 2.9 nM
2 Ki = 6 nM
CP0086179
[5-chloro-4-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-methoxyphenyl]-morpholin-4-ylmethanone
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C19H21ClF3N5O3
 2
1 Ki = 3 nM
2 Ki = 3.4 nM
CP0301155
[5-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-4-methoxypyridin-2-yl]-morpholin-4-ylmethanone
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C18H21F3N6O3
 1
1 Ki = 3 nM
CP0179672
5-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-(2-hydroxy-2-methylpropyl)-6-methoxy-3H-isoindol-1-one
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C20H24F3N5O3
 2
1 Ki = 3 nM
2 Ki = 4 nM
CP0267368
[5-fluoro-2-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
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C18H19F4N5O3
 2
1 Ki = 4.8 nM
2 Ki = 7 nM
CP0301157
[4-[(5-bromo-4-methoxypyrimidin-2-yl)amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
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C17H19BrN4O4
 1
1 Ki = 5 nM
CP0239078
[5-chloro-2-methyl-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
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C18H19ClF3N5O2
 1
1 Ki = 7 nM
CP0061269
2-N-[2-chloro-4-(1-methyltetrazol-5-yl)phenyl]-4-N-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
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C14H12ClF3N8
 2
1 Ki = 7 nM
2 Ki = 8 nM
CP0179678
[4-[(5-chloro-4-methoxypyrimidin-2-yl)amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
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C17H19ClN4O4
 2
1 Ki = 9 nM
2 Ki = 10.4 nM
CP0335187
2-N-[4-methoxy-6-(oxan-4-yl)pyridin-3-yl]-4-N-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
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C17H20F3N5O2
 1
1 Ki = 9 nM
CP0339216
[2-fluoro-3-methoxy-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]phenyl]-morpholin-4-ylmethanone
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C18H19F4N5O3
 2
1 Ki = 12 nM
2 Ki = 14.5 nM
CP0087686
[4-[[5-fluoro-4-(methylamino)pyrimidin-2-yl]amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
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C17H20FN5O3
 2
1 Ki = 58 nM
2 Ki = 71 nM
Clinical Information about the Protein
Target 1 ( Leucine-rich repeat kinase 2 (LRRK2) )
Target Type Clinical trial Target
Target 2 ( Leucine-rich repeat kinase 2 G2019S mutant (LRRK2 G2019S) )
Target Type Patented-recorded Target
Target 3 ( Leucine-rich repeat kinase 2 S935 phosphorylation (LRRK2 pS935) )
Target Type Patented-recorded Target
Target 4 ( Leucine-rich repeat serine/threonine-protein kinase 2 messenger RNA (LRRK2 mRNA) )
Target Type Clinical trial Target
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06768 Leucine-rich repeat serine/threonine-protein kinase 2 Mus musculus, Mouse