Protein Information

General Information of the Protein

Protein ID	PT00865
Protein Name	Serine/threonine-protein kinase Chk1
Secondarily Protein Name	CHK1 checkpoint homolog Cell cycle checkpoint kinase Checkpoint kinase-1
Gene Name	CHEK1
Secondarily Gene Name	CHK1
Sequence	MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINKMLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVYLHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLKRREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLALLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDFSPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLLGTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRRNNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Kinase > Protein Kinase > CAMK protein kinase group > CAMK protein kinase CAMK1 family > CAMK protein kinase CHK1 subfamily
Function	Serine/threonine-protein kinase which is required for checkpoint-mediated cell cycle arrest and activation of DNA repair in response to the presence of DNA damage or unreplicated DNA (PubMed:11535615, PubMed:12446774, PubMed:12399544, PubMed:14559997, PubMed:14988723, PubMed:15311285, PubMed:15665856, PubMed:15650047, PubMed:32357935). May also negatively regulate cell cycle progression during unperturbed cell cycles (PubMed:11535615, PubMed:12446774, PubMed:12399544, PubMed:14559997, PubMed:14988723, PubMed:15311285, PubMed:15665856, PubMed:15650047). This regulation is achieved by a number of mechanisms that together help to preserve the integrity of the genome (PubMed:11535615, PubMed:12446774, PubMed:12399544, PubMed:14559997, PubMed:14988723, PubMed:15311285, PubMed:15665856, PubMed:15650047). Recognizes the substrate consensus sequence [R-X-X-S/T] (PubMed:11535615, PubMed:12446774, PubMed:12399544, PubMed:14559997, PubMed:14988723, PubMed:15311285, PubMed:15665856, PubMed:15650047). Binds to and phosphorylates CDC25A, CDC25B and CDC25C (PubMed:9278511, PubMed:12676583, PubMed:14681206, PubMed:12676925, PubMed:12759351, PubMed:19734889, PubMed:14559997). Phosphorylation of CDC25A at 'Ser-178' and 'Thr-507' and phosphorylation of CDC25C at 'Ser-216' creates binding sites for 14-3-3 proteins which inhibit CDC25A and CDC25C (PubMed:9278511). Phosphorylation of CDC25A at 'Ser-76', 'Ser-124', 'Ser-178', 'Ser-279' and 'Ser-293' promotes proteolysis of CDC25A (PubMed:9278511, PubMed:12676583, PubMed:14681206, PubMed:12676925, PubMed:12759351, PubMed:19734889). Phosphorylation of CDC25A at 'Ser-76' primes the protein for subsequent phosphorylation at 'Ser-79', 'Ser-82' and 'Ser-88' by NEK11, which is required for polyubiquitination and degradation of CDCD25A (PubMed:9278511, PubMed:19734889, PubMed:20090422). Inhibition of CDC25 leads to increased inhibitory tyrosine phosphorylation of CDK-cyclin complexes and blocks cell cycle progression (PubMed:9278511). Also phosphorylates NEK6 (PubMed:18728393). Binds to and phosphorylates RAD51 at 'Thr-309', which promotes the release of RAD51 from BRCA2 and enhances the association of RAD51 with chromatin, thereby promoting DNA repair by homologous recombination (PubMed:15665856). Phosphorylates multiple sites within the C-terminus of TP53, which promotes activation of TP53 by acetylation and promotes cell cycle arrest and suppression of cellular proliferation (PubMed:10673501, PubMed:15659650, PubMed:16511572). Also promotes repair of DNA cross-links through phosphorylation of FANCE (PubMed:17296736). Binds to and phosphorylates TLK1 at 'Ser-743', which prevents the TLK1-dependent phosphorylation of the chromatin assembly factor ASF1A (PubMed:12660173, PubMed:12955071). This may enhance chromatin assembly both in the presence or absence of DNA damage (PubMed:12660173, PubMed:12955071). May also play a role in replication fork maintenance through regulation of PCNA (PubMed:18451105). May regulate the transcription of genes that regulate cell-cycle progression through the phosphorylation of histones (By similarity). Phosphorylates histone H3.1 (to form H3T11ph), which leads to epigenetic inhibition of a subset of genes (By similarity). May also phosphorylate RB1 to promote its interaction with the E2F family of transcription factors and subsequent cell cycle arrest (PubMed:17380128). Phosphorylates SPRTN, promoting SPRTN recruitment to chromatin (PubMed:31316063). Reduces replication stress and activates the G2/M checkpoint, by phosphorylating and inactivating PABIR1/FAM122A and promoting the serine/threonine-protein phosphatase 2A-mediated dephosphorylation and stabilization of WEE1 levels and activity (PubMed:33108758). Show/Hide
Uniprot ID	Primary ID: O14757 Secondarily ID: A8K934 B4DDD0 B4DSK3 B5BTY6 F5H7S4 H2BI51 Show/Hide
HGNC ID	HGNC:1925
Subcellular Location	Nucleus Chromosome Cytoplasm Cytoplasm Cytoskeleton Microtubule organizing center Centrosome

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: CL000382 , CA46

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0484216 Compound Info	4'-[5-(4-pyrrolidin-1-ylmethyl-phenylamino)-1H-pyrazol-3-yl]-biphenyl-2,4-diol Show/Hide	C26H26N4O2	1
1	EC50 = 41 nM Bioactivity Info	TI LI LO TS
CP0427363 Compound Info	4'-{5-[4-(dimethylamino-methyl)-phenylamino]-2H-pyrazol-3-yl}-biphenyl-2,4-diol Show/Hide	C24H24N4O2	1
1	EC50 = 58 nM Bioactivity Info	TI LI LO TS
CP0449355 Compound Info	4'-[5-(4-cyclopropylaminomethyl-phenylamino)-2H-pyrazol-3-yl]-biphenyl-2,4-diol Show/Hide	C25H24N4O2	1
1	EC50 = 60 nM Bioactivity Info	TI LI LO TS
CP0038189 Compound Info	4'-{5-[4-(isopropylamino-methyl)-phenylamino]-2H-pyrazol-3-yl}-biphenyl-2,4-diol Show/Hide	C25H26N4O2	1
1	EC50 = 70 nM Bioactivity Info	TI LI LO TS
CP0525945 Compound Info	4'-[5-(6-piperidin-1-ylmethyl-pyridin-3-ylamino)-1H-pyrazol-3-yl]-biphenyl-2,4-diol Show/Hide	C26H27N5O2	1
1	EC50 = 150 nM Bioactivity Info	TI LI LO TS
CP0427362 Compound Info	4'-(5-{6-[(cyclopropylmethyl-amino)-methyl]-pyridin-3-ylamino}-1H-pyrazol-3-yl)-biphenyl-2,4-diol Show/Hide	C25H25N5O2	1
1	EC50 = 165 nM Bioactivity Info	TI LI LO TS
CP0433780 Compound Info	4'-{5-[6-(sec-butylamino-methyl)-pyridin-3-ylamino]-1H-pyrazol-3-yl}-biphenyl-2,4-diol Show/Hide	C25H27N5O2	1
1	EC50 = 230 nM Bioactivity Info	TI LI LO TS
CP0505229 Compound Info	4'-(5-phenylamino-2H-pyrazol-3-yl)-biphenyl-2,4-diol Show/Hide	C21H17N3O2	1
1	EC50 = 500 nM Bioactivity Info	TI LI LO TS
CP0484215 Compound Info	3-(1H-benzo[d]imidazol-2-yl)-N-(2,4-dihydroxyphenyl)-1H-indazole-6-carboxamide Show/Hide	C21H15N5O3	1
1	EC50 = 550 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000017 , HeLa

Cell Line Info

Cell Line ID: CL000162 , HeLa S3

Cell Line Info

Cell Line ID: CL000007 , HT-29

Cell Line Info

Cell Line ID: CL000095 , NCI-H1299

Cell Line Info

Cell Line ID: CL000012 , Sf21

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000104 , SW620

Cell Line Info

Cell Line ID: CL000043 , U2OS

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0004106 Compound Info	(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one Show/Hide	C28H26N4O3	8
1	IC50 < 0.1 nM
2	IC50 = 0.142 nM
3	IC50 = 0.16 nM
4	IC50 = 0.186 nM
5	IC50 < 0.5 nM
6	IC50 = 2.1 nM
7	IC50 = 9.5 nM
8	Kd = 3.2 nM
CP0126650 Compound Info	5-methyl-8-(1H-pyrrol-2-yl)-[1,2,4]triazolo[4,3-a]quinolin-1(2H)-one Show/Hide	C15H12N4O	1
1	IC50 = 0.1 nM
CP0153182 Compound Info	4-(1-methylpyrazol-4-yl)-12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene Show/Hide	C26H26N6	1
1	IC50 = 0.31 nM
CP0343610 Compound Info	(S)-3-(1H-benzo[d]imidazol-2-yl)-6-chloro-4-(quinuclidin-3-ylamino)quinolin-2(1H)-one Show/Hide	C23H22ClN5O	1
1	IC50 = 0.32 nM
CP0347609 Compound Info	2-oxo-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)-1,2-dihydroquinoline-6-carboxamide Show/Hide	C24H24N4O2	1
1	IC50 = 0.34 nM
CP0060053 Compound Info	5-[12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-4-yl]-1,3-oxazole Show/Hide	C25H23N5O	1
1	IC50 = 0.46 nM
CP0554617 Compound Info	methyl 6-[(5-cyanopyrazin-2-yl)amino]-4-[[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]amino]pyridine-3-carboxylate Show/Hide	C20H23N7O2	1
1	IC50 = 0.5 nM
CP0554618 Compound Info	5-[[5-(5-methyl-1,3-thiazol-2-yl)-4-[[(2R)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C19H20N8OS	1
1	IC50 = 0.5 nM
CP0554619 Compound Info	1137478-52-4 Show/Hide	C20H23N7O2	1
1	IC50 = 0.5 nM
CP0195264 Compound Info	2-(2-hydroxyethoxy)-3-methoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C23H21N3O7	1
1	IC50 = 0.58 nM
CP0295944 Compound Info	2,3-dimethoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C22H19N3O6	1
1	IC50 = 0.6 nM
CP0210351 Compound Info	6-(isothiazol-4-yl)-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)quinolin-2(1H)-one Show/Hide	C26H24N4OS	1
1	IC50 = 0.64 nM
CP0172391 Compound Info	3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)-6-(1H-pyrazol-4-yl)quinolin-2(1H)-one Show/Hide	C26H25N5O	1
1	IC50 = 0.65 nM
CP0256905 Compound Info	2-(4-hydroxybutoxy)-3-methoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C25H25N3O7	1
1	IC50 = 0.7 nM
CP0342012 Compound Info	3-(5-((4-(aminomethyl)piperidin-1-yl)methyl)-1H-indol-2-yl)-2-oxo-1,2-dihydroquinoline-6-carboxamide Show/Hide	C25H27N5O2	1
1	IC50 = 0.7 nM
CP0051735 Compound Info	3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)-6-(1H-1,2,3-triazol-1-yl)quinolin-2(1H)-one Show/Hide	C25H24N6O	1
1	IC50 = 0.74 nM
CP0764664 Compound Info	3-(5-Ethyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile Show/Hide	C20H17N5S	1
1	IC50 = 0.78 nM
CP0172389 Compound Info	3-(5-(morpholinomethyl)-1H-indol-2-yl)-6-(1H-pyrazol-4-yl)quinolin-2(1H)-one Show/Hide	C25H23N5O2	1
1	IC50 = 0.83 nM
CP0295941 Compound Info	2-hydroxy-3-methoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C21H17N3O6	1
1	IC50 = 0.9 nM
CP0240739 Compound Info	5-[[5-(1-methylpyrazol-4-yl)-4-[[(2R)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C19H21N9O	1
1	IC50 = 0.9 nM
CP0115012 Compound Info	2-[12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-4-yl]-1,3,4-oxadiazole Show/Hide	C24H22N6O	1
1	IC50 = 0.95 nM
CP0348656 Compound Info	12-[4-(piperidin-1-ylmethyl)phenyl]-4-pyridin-3-yl-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene Show/Hide	C27H25N5	1
1	IC50 = 0.95 nM
CP0256904 Compound Info	2-(3-aminopropoxy)-3-methoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C24H24N4O6	1
1	IC50 = 0.98 nM
CP0352392 Compound Info	3-(5-((4-fluoropiperidin-1-yl)methyl)-1H-indol-2-yl)-6-(1H-pyrazol-4-yl)quinolin-2(1H)-one Show/Hide	C26H24FN5O	1
1	IC50 = 1 nM
CP0057266 Compound Info	5-[[4-(methylamino)-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]-3-[(3S)-pyrrolidin-3-yl]oxypyrazine-2-carbonitrile Show/Hide	C19H21N9O	1
1	IC50 < 1 nM
CP0087827 Compound Info	5-[[4-methoxy-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]-3-[(3R)-pyrrolidin-3-yl]oxypyrazine-2-carbonitrile Show/Hide	C19H20N8O2	1
1	IC50 < 1 nM
CP0260556 Compound Info	5-[[4-(methylamino)-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]-3-[(3R)-pyrrolidin-3-yl]oxypyrazine-2-carbonitrile Show/Hide	C19H21N9O	1
1	IC50 < 1 nM
CP0058804 Compound Info	12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C23H21N5	1
1	IC50 = 1 nM
CP0240733 Compound Info	CHEMBL4789854 Show/Hide	C19H21N7O2	1
1	IC50 = 1 nM
CP0347607 Compound Info	6-(1-methyl-1H-pyrazol-4-yl)-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)quinolin-2(1H)-one Show/Hide	C27H27N5O	1
1	IC50 = 1.1 nM
CP0181972 Compound Info	4-[12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-4-yl]-1,2-oxazole Show/Hide	C25H23N5O	1
1	IC50 = 1.1 nM
CP0017298 Compound Info	12-[4-(4-methylpiperazin-1-yl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C22H20N6	1
1	IC50 = 1.3 nM
CP0058257 Compound Info	5-[12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-4-yl]-1,3-thiazole Show/Hide	C25H23N5S	1
1	IC50 = 1.3 nM
CP0228418 Compound Info	5-[[4-[[(2R)-morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile Show/Hide	C16H16F3N7O	2
1	IC50 = 1.3 nM
2	IC50 = 2 nM
CP0651903 Compound Info	3-(4-((4-Hydroxypiperidin-1-yl)methyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile Show/Hide	C23H21N5O	1
1	IC50 = 1.8 nM
CP0361644 Compound Info	3-(3-hydroxypropyl)-2-methoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C24H23N3O6	1
1	IC50 = 1.9 nM
CP0573640 Compound Info	12-[3-(4-methylpiperazin-1-yl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C22H20N6	1
1	IC50 = 1.9 nM
CP0719003 Compound Info	(R)-3-(4-((3-Hydroxypiperidin-1-yl)methyl)phenyl)-9H-pyrrolo-[2,3-b:5,4-c']dipyridine-6-carbonitrile Show/Hide	C23H21N5O	1
1	IC50 = 1.9 nM
CP0477874 Compound Info	5-[[5-chloro-4-[[(2R)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C15H16ClN7O	1
1	IC50 = 1.9 nM
CP0065184 Compound Info	8-(1,1-dioxo-1l6-isothiazolidin-2-yl)-3-(3-methoxy-4-nitrophenyl)-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one Show/Hide	C23H22N4O4S	1
1	IC50 = 2 nM
CP0333593 Compound Info	3-[3-(3-methoxy-4-nitrophenyl)-11-oxo-10,11-dihydro-5Hdibenzo[b,e][1,4]diazepin-8-yl]-N,N-dimethylpropanamide Show/Hide	C25H26N4O3	1
1	IC50 = 2 nM
CP0370390 Compound Info	3-(5-((4-(2-methoxyacetyl)piperazin-1-yl)methyl)-1H-indol-2-yl)-6-(1H-pyrazol-4-yl)quinolin-2(1H)-one Show/Hide	C28H28N6O3	1
1	IC50 = 2.1 nM
CP0762094 Compound Info	3-(4-(((2R,6S)-2,6-Dimethylpiperidin-1-yl)methyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile Show/Hide	C25H25N5	1
1	IC50 = 2.1 nM
CP0553237 Compound Info	5-[[5-[2-(1-hydroxycyclopentyl)ethynyl]-4-[[(2S)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C22H25N7O2	1
1	IC50 = 2.1 nM
CP0317168 Compound Info	1137477-07-6 Show/Hide	C17H19N7O3	1
1	IC50 = 2.2 nM
CP0548558 Compound Info	1137478-46-6 Show/Hide	C20H23N7O2	1
1	IC50 = 2.2 nM
CP0194072 Compound Info	1-[4-({2-[6-(1H-1,2,3,4-tetrazol-5-yl)-1H-indazol-3-yl]-1H-indol-5-yl}methyl)piperazin-1-yl]ethan-1-one Show/Hide	C23H23N9O	1
1	IC50 = 2.3 nM
CP0044962 Compound Info	12-[4-(piperidin-1-ylmethyl)phenyl]-4-pyrazin-2-yl-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene Show/Hide	C26H24N6	1
1	IC50 = 2.3 nM
CP0764666 Compound Info	3-(2-Ethyl-1,2,3,4-tetrahydroisoquinolin-6-yl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile Show/Hide	C22H19N5	1
1	IC50 = 2.3 nM
CP0352393 Compound Info	3-(5-((4-acetylpiperazin-1-yl)methyl)-1H-indol-2-yl)-6-(1H-pyrazol-4-yl)quinolin-2(1H)-one Show/Hide	C27H26N6O2	1
1	IC50 = 2.5 nM
CP0731627 Compound Info	3-(4-((2-Oxa-7-azaspiro[3.5]nonan-7-yl)methyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']-dipyridine-6-carbonitrile Show/Hide	C25H23N5O	1
1	IC50 = 2.5 nM
CP0321414 Compound Info	2-(3-hydroxypropyl)-3-methoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C24H23N3O6	1
1	IC50 = 2.6 nM
CP0036465 Compound Info	6-bromo-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)quinolin-2(1H)-one Show/Hide	C23H22BrN3O	1
1	IC50 = 2.9 nM
CP0145928 Compound Info	3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[5-(3-hydroxy-3-methylbut-1-ynyl)-4-(methylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C21H27N7O2	1
1	IC50 = 2.9 nM
CP0176865 Compound Info	12-[4-(piperidin-1-ylmethyl)phenyl]-4-pyridazin-4-yl-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene Show/Hide	C26H24N6	1
1	IC50 = 2.9 nM
CP0477871 Compound Info	methyl 6-[(5-cyanopyrazin-2-yl)amino]-4-[(1-methylpiperidin-4-yl)amino]pyridine-3-carboxylate Show/Hide	C18H21N7O2	1
1	IC50 = 2.9 nM
CP0051736 Compound Info	3-(5-((4-acetylpiperazin-1-yl)methyl)-1H-indol-2-yl)-6-(1-methyl-1H-pyrazol-4-yl)quinolin-2(1H)-one Show/Hide	C28H28N6O2	1
1	IC50 = 3 nM
CP0333594 Compound Info	methyl 2-[9-(4-amino-3-methoxyphenyl)-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepin-3-yl]acetate Show/Hide	C23H21N3O4	1
1	IC50 = 3 nM
CP0103447 Compound Info	3-methoxy-2-[2-(2-methoxyethoxy)ethoxy]-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C26H27N3O8	1
1	IC50 = 3.1 nM
CP0070066 Compound Info	3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[4-(methylamino)-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C20H25N9O	1
1	IC50 = 3.1 nM
CP0354070 Compound Info	1137478-45-5 Show/Hide	C19H21N9O	1
1	IC50 = 3.2 nM
CP0361645 Compound Info	Chk1_152 Show/Hide	C25H25N3O6	1
1	IC50 = 3.4 nM
CP0283373 Compound Info	5-[[4-(methylamino)-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]-3-[(3S)-1-methylpyrrolidin-3-yl]oxypyrazine-2-carbonitrile Show/Hide	C20H23N9O	1
1	IC50 = 3.4 nM
CP0256901 Compound Info	2-(2-hydroxyethyl)-3-methoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C23H21N3O6	1
1	IC50 = 3.5 nM
CP0045636 Compound Info	2-(5-methoxy-3-oxo-1H-isoindol-2-yl)-N-(4-piperazin-1-ylpyridin-3-yl)-1,3-thiazole-4-carboxamide Show/Hide	C22H22N6O3S	1
1	IC50 = 3.7 nM
CP0103446 Compound Info	2-(3-hydroxy-3-methylbutyl)-3-methoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C26H27N3O6	1
1	IC50 = 4 nM
CP0256903 Compound Info	3-methoxy-9-(3-methoxy-4-nitrophenyl)-2-[(2-methyl-1,3-thiazol-4-yl)methoxy]-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C26H22N4O6S	1
1	IC50 = 4 nM
CP0215697 Compound Info	3-(5-((4-(aminomethyl)piperidin-1-yl)methyl)-1H-indol-2-yl)-2-oxo-1,2-dihydroquinoline-6-carbonitrile Show/Hide	C25H25N5O	1
1	IC50 = 4 nM
CP0065183 Compound Info	3-(3-methoxy-4-nitrophenyl)-8-(2-oxopyrrolidin-1-yl)-5,10-dihydro-11H-dibenzo[b,e][1,4]diazepin-11-one Show/Hide	C24H22N4O3	1
1	IC50 = 4 nM
CP0286129 Compound Info	3-(4-amino-3-methoxy-phenyl)-7-morpholin-4-yl-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one Show/Hide	C24H24N4O3	1
1	IC50 = 4 nM
CP0306005 Compound Info	(S)-2-phenyl-4-(piperidin-3-ylamino)thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C19H20N4OS	2
1	IC50 = 4 nM
2	IC50 = 7 nM
CP0123581 Compound Info	2-(1H-indol-5-yl)-N-(2-piperazin-1-ylphenyl)-1,3-thiazole-4-carboxamide Show/Hide	C22H21N5OS	1
1	IC50 = 4 nM
CP0156366 Compound Info	12-[4-(4-methylpiperazin-1-yl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene-4-carboxylic acid Show/Hide	C22H21N5O2	1
1	IC50 = 4.1 nM
CP0707835 Compound Info	3-(4-(((3R,5S)-3,5-Dimethylpiperidin-1-yl)methyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']-dipyridine-6-carbonitrile Show/Hide	C25H25N5	1
1	IC50 = 4.2 nM
CP0529683 Compound Info	6-(1H-imidazol-1-yl)-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)quinolin-2(1H)-one Show/Hide	C26H25N5O	1
1	IC50 = 4.3 nM
CP0114987 Compound Info	12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene-4-carboxamide Show/Hide	C23H23N5O	1
1	IC50 = 4.3 nM
CP0161532 Compound Info	5-[[4-(methylamino)-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]-3-[(3R)-1-methylpyrrolidin-3-yl]oxypyrazine-2-carbonitrile Show/Hide	C20H23N9O	1
1	IC50 = 4.4 nM
CP0687999 Compound Info	3-(4-((4,4-Dimethylpiperidin-1-yl)methyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile Show/Hide	C25H25N5	1
1	IC50 = 4.4 nM
CP0172392 Compound Info	2-oxo-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)-1,2-dihydroquinoline-6-carbonitrile Show/Hide	C24H22N4O	1
1	IC50 = 4.6 nM
CP0567388 Compound Info	5-[[5-(1-methylindazol-5-yl)-4-[[(2R)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C23H23N9O	1
1	IC50 = 4.6 nM
CP0567379 Compound Info	5-[[5-[(E)-4-hydroxybut-1-enyl]-4-(piperidin-4-ylmethylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C20H25N7O	1
1	IC50 = 4.7 nM
CP0215193 Compound Info	3-methoxy-9-(3-methoxy-4-nitrophenyl)-2-(oxan-2-ylmethoxy)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C27H27N3O7	1
1	IC50 = 4.8 nM
CP0114061 Compound Info	2-(1-benzothiophen-5-yl)-N-(2-piperazin-1-ylphenyl)-1,3-thiazole-4-carboxamide Show/Hide	C22H20N4OS2	1
1	IC50 = 5 nM
CP0196834 Compound Info	2-(4-phenoxyphenyl)-N-(2-piperazin-1-ylphenyl)-1,3-thiazole-4-carboxamide Show/Hide	C26H24N4O2S	1
1	IC50 = 5 nM
CP0689009 Compound Info	3-(4-((4-Fluoropiperidin-1-yl)methyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile Show/Hide	C23H20FN5	1
1	IC50 = 5 nM
CP0145132 Compound Info	AZD7762 Show/Hide	C17H19FN4O2S	3
1	IC50 = 5 nM
2	IC50 = 6 nM
3	IC50 = 7.89 nM
CP0251940 Compound Info	12-[4-(piperidin-1-ylmethyl)phenyl]-4-pyrimidin-5-yl-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene Show/Hide	C26H24N6	1
1	IC50 = 5.1 nM
CP0251044 Compound Info	5-[[5-ethynyl-4-[[(2S)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C17H17N7O	1
1	IC50 = 5.2 nM
CP0537177 Compound Info	5-[[5-(3-chlorophenyl)-4-[[(2R)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C21H20ClN7O	1
1	IC50 = 5.2 nM
CP0769320 Compound Info	3-(6-(Piperidin-1-ylmethyl)pyridin-3-yl)-9H-pyrrolo[2,3-b:5,4-c']-dipyridine-6-carbonitrile Show/Hide	C22H20N6	1
1	IC50 = 5.3 nM
CP0122409 Compound Info	methyl 6-[[5-cyano-6-[(3R)-pyrrolidin-3-yl]oxypyrazin-2-yl]amino]-4-(methylamino)pyridine-3-carboxylate Show/Hide	C17H19N7O3	1
1	IC50 = 5.4 nM
CP0523734 Compound Info	3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)-6-(1H-pyrazol-3-yl)quinolin-2(1H)-one Show/Hide	C26H25N5O	1
1	IC50 = 5.6 nM
CP0065182 Compound Info	2-[3-(3-methoxy-4-nitrophenyl)-11-oxo-10,11-dihydro-5Hdibenzo[b,e][1,4]diazepin-8-yl]-N,N-dimethylacetamide Show/Hide	C24H24N4O3	1
1	IC50 = 6 nM
CP0185338 Compound Info	7-amino-3-(4-amino-3-methoxy-phenyl)-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one Show/Hide	C20H18N4O2	1
1	IC50 = 6 nM
CP0333592 Compound Info	2-[3-(3-methoxy-4-nitrophenyl)-11-oxo-10,11-dihydro-5Hdibenzo[b,e][1,4]diazepin-7-yl]-N,N-dimethylacetamide Show/Hide	C24H24N4O3	1
1	IC50 = 6 nM
CP0419808 Compound Info	4-[[(3S)-piperidin-3-yl]amino]-2-thiophen-3-ylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C17H18N4OS2	1
1	IC50 = 6 nM
CP0463930 Compound Info	4-[[(2R,3S)-2-methylpiperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C20H22N4OS	1
1	IC50 = 6 nM
CP0558615 Compound Info	2-(1-methylpyrazol-4-yl)-4-[[(3S)-piperidin-3-yl]amino]thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C17H20N6OS	1
1	IC50 = 6 nM
CP0071665 Compound Info	5-[(8-chloroisoquinolin-3-yl)amino]-3-[(2R)-1-(dimethylamino)propan-2-yl]oxypyrazine-2-carbonitrile Show/Hide	C19H19ClN6O	2
1	IC50 = 6.1 nM
2	IC50 = 13 nM
CP0039009 Compound Info	3-(4'-HYDROXYBIPHENYL-4-YL)-N-(4-HYDROXYCYCLOHEXYL)-1,4-DIHYDROINDENO[1,2-C]PYRAZOLE-6-CARBOXAMIDE Show/Hide	C29H27N3O3	2
1	IC50 = 6.2 nM
2	Ki = 6.31 nM
CP0260555 Compound Info	5-[[4-methoxy-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]-3-[(3R)-1-methylpyrrolidin-3-yl]oxypyrazine-2-carbonitrile Show/Hide	C20H22N8O2	1
1	IC50 = 6.3 nM
CP0370389 Compound Info	6-(2-methyl-2H-tetrazol-5-yl)-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)quinolin-2(1H)-one Show/Hide	C25H25N7O	1
1	IC50 = 6.4 nM
CP0240738 Compound Info	5-[[5-(3-fluorophenyl)-4-[[(2R)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C21H20FN7O	1
1	IC50 = 6.4 nM
CP0355909 Compound Info	1137478-38-6 Show/Hide	C22H23N7O2	1
1	IC50 = 6.4 nM
CP0020879 Compound Info	2-[3-(3-methoxy-4-nitrophenyl)-11-oxo-10,11-dihydro-5Hdibenzo[b,e][1,4]diazepin-8-yl]-2-methyl-N-(4-morpholin-4-ylphenyl)propanamide Show/Hide	C34H35N5O4	1
1	IC50 = 6.7 nM
CP0136934 Compound Info	Chk1_136 Show/Hide	C27H22N4O6	1
1	IC50 = 6.8 nM
CP0021747 Compound Info	2-[3-(3-methoxy-4-nitrophenyl)-11-oxo-10,11-dihydro-5Hdibenzo[b,e][1,4]diazepin-8-yl]-N-[4-(4-morpholinyl)phenyl]acetamide Show/Hide	C32H31N5O4	1
1	IC50 = 7 nM
CP0042443 Compound Info	(S)-1-(5-phenyl-3-(piperidin-3-ylcarbamoyl)thiophen-2-yl)urea Show/Hide	C17H20N4O2S	1
1	IC50 = 7 nM
CP0450695 Compound Info	2-(1-benzothiophen-2-yl)-N-(2-piperazin-1-ylphenyl)-1,3-thiazole-4-carboxamide Show/Hide	C22H20N4OS2	1
1	IC50 = 7 nM
CP0161533 Compound Info	methyl 6-[[5-cyano-6-[(2R)-1-(dimethylamino)propan-2-yl]oxypyrazin-2-yl]amino]-4-(methylamino)pyridine-3-carboxylate Show/Hide	C18H23N7O3	1
1	IC50 = 7 nM
CP0552175 Compound Info	CHEMBL4756720 Show/Hide	C21H25N7O2	1
1	IC50 = 7 nM
CP0251043 Compound Info	5-[[5-cyclopropyl-4-[[(2S)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C18H21N7O	1
1	IC50 = 7.4 nM
CP0018695 Compound Info	3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[4-methoxy-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C20H24N8O2	1
1	IC50 = 7.7 nM
CP0422380 Compound Info	3-[3-methoxy-9-(3-methoxy-4-nitrophenyl)-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepin-2-yl]-N,N-dimethylpropanamide Show/Hide	C26H26N4O6	1
1	IC50 = 7.9 nM
CP0277183 Compound Info	3-methoxy-9-(3-methoxy-4-nitrophenyl)-2-(2-morpholin-4-ylethoxy)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C27H28N4O7	1
1	IC50 = 8.1 nM
CP0548557 Compound Info	5-[[5-(2-methylindazol-5-yl)-4-[[(2R)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C23H23N9O	1
1	IC50 = 8.5 nM
CP0169779 Compound Info	methyl 6-[[5-cyano-6-[(3R)-pyrrolidin-3-yl]oxypyrazin-2-yl]amino]-4-(dimethylamino)pyridine-3-carboxylate Show/Hide	C18H21N7O3	1
1	IC50 = 8.8 nM
CP0558634 Compound Info	6-[(5-cyanopyrazin-2-yl)amino]-N-ethyl-4-(piperidin-4-ylmethylamino)pyridine-3-carboxamide Show/Hide	C19H24N8O	1
1	IC50 = 8.8 nM
CP0348336 Compound Info	3-ethyl-2-methoxy-9-(3-methoxy-4-nitrophenyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C23H21N3O5	1
1	IC50 = 9 nM
CP0538858 Compound Info	2-(3-fluorophenyl)-4-[[(3S)-piperidin-3-yl]amino]-1H-indole-7-carboxamide Show/Hide	C20H21FN4O	1
1	IC50 = 9 nM
CP0251948 Compound Info	12-[4-(piperidin-1-ylmethyl)phenyl]-4-pyridin-4-yl-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene Show/Hide	C27H25N5	1
1	IC50 = 9.1 nM
CP0058806 Compound Info	12-[4-[(3,3-dimethylpiperidin-1-yl)methyl]phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C25H25N5	1
1	IC50 = 9.4 nM
CP0065181 Compound Info	3-[3-(3-methoxy-4-nitrophenyl)-11-oxo-10,11-dihydro-5Hdibenzo[b,e][1,4]diazepin-8-yl]-N-(4-morpholin-4-ylphenyl)propanamide Show/Hide	C33H33N5O4	1
1	IC50 = 10 nM
CP0195563 Compound Info	2-[3-(3-methoxy-4-nitrophenyl)-11-oxo-10,11-dihydro-5Hdibenzo[b,e][1,4]diazepin-7-yl]-2-methyl-N-(4-morpholin-4-ylphenyl)propanamide Show/Hide	C34H35N5O4	1
1	IC50 = 10 nM
CP0088592 Compound Info	8-(4-(hydroxymethyl)phenyl)-5-methyl-[1,2,4]triazolo[4,3-a]quinolin-1(2H)-one Show/Hide	C18H15N3O2	1
1	IC50 = 10 nM
CP0558622 Compound Info	4-[[(3S,4S)-4-hydroxypiperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C19H20N4O2S	1
1	IC50 = 10 nM
CP0651902 Compound Info	3-(4-(2-(Piperidin-1-yl)propan-2-yl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile Show/Hide	C25H25N5	1
1	IC50 = 10.2 nM
CP0213191 Compound Info	8-hydroxy-3-(3-methoxy-4-nitrophenyl)-5H-dibenzo[b,e][1,4]-diazepin-11(10H)-one Show/Hide	C20H17N3O3	1
1	IC50 = 11 nM
CP0270435 Compound Info	3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[5-ethynyl-4-(methylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C18H21N7O	1
1	IC50 = 11 nM
CP0317167 Compound Info	1168103-91-0 Show/Hide	C22H23N7O2	1
1	IC50 = 11 nM
CP0552172 Compound Info	methyl 6-[(5-cyanopyrazin-2-yl)amino]-4-(2-piperidin-4-ylethylamino)pyridine-3-carboxylate Show/Hide	C19H23N7O2	1
1	IC50 = 11 nM
CP0256900 Compound Info	methyl 2-methoxy-9-(3-methoxy-4-nitrophenyl)-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepine-3-carboxylate Show/Hide	C23H19N3O7	1
1	IC50 = 11.2 nM
CP0185516 Compound Info	12-[4-(hydroxymethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C18H12N4O	1
1	IC50 = 11.4 nM
CP0841492 Compound Info	3-(4-((4-Cyanopiperidin-1-yl)methyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile Show/Hide	C24H20N6	1
1	IC50 = 11.6 nM
CP0214767 Compound Info	4-[[(2S,3S,6R)-2,6-dimethylpiperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C21H24N4OS	1
1	IC50 = 12 nM
CP0407242 Compound Info	2-(3-fluorophenyl)-4-[[(3S)-piperidin-3-yl]amino]thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C19H19FN4OS	1
1	IC50 = 12 nM
CP0477869 Compound Info	5-[[5-(3-hydroxy-3-methylbut-1-ynyl)-4-(piperidin-4-ylmethylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C21H25N7O	1
1	IC50 = 12 nM
CP0489024 Compound Info	5-[[5-(3,5-difluorophenyl)-4-[[(2R)-morpholin-2-yl]methylamino]pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C21H19F2N7O	1
1	IC50 = 12 nM
CP0273724 Compound Info	N-[3-(4-cyano-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-12-yl)phenyl]acetamide Show/Hide	C19H13N5O	1
1	IC50 = 13.5 nM
CP0788365 Compound Info	3-(4-(Piperidin-1-ylmethyl)thiazol-2-yl)-9H-pyrrolo[2,3-b:5,4-c']-dipyridine-6-carbonitrile Show/Hide	C20H18N6S	1
1	IC50 = 13.6 nM
CP0659565 Compound Info	3-(4-(Morpholinomethyl)phenyl)-9H-pyrrolo[2,3-b:5,4-c']-dipyridine-6-carbonitrile Show/Hide	C22H19N5O	1
1	IC50 = 13.9 nM
CP0194220 Compound Info	3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)-6-(2H-1,2,3-triazol-2-yl)quinolin-2(1H)-one Show/Hide	C25H24N6O	1
1	IC50 = 14 nM
CP0270494 Compound Info	8-methoxy-3-(3-methoxy-4-nitrophenyl)-5H-dibenzo[b,e][1,4]-diazepin-11(10H)-one Show/Hide	C21H19N3O3	1
1	IC50 = 14 nM
CP0519451 Compound Info	2-(1-benzylpyrazol-4-yl)-4-[[(3S)-piperidin-3-yl]amino]thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C23H24N6OS	1
1	IC50 = 14 nM
CP0115009 Compound Info	12-(1H-imidazol-2-yl)-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C14H8N6	1
1	IC50 = 14.7 nM
CP0300580 Compound Info	2-(4-chlorophenyl)-4-[[(3S)-piperidin-3-yl]amino]-1H-indole-7-carboxamide Show/Hide	C20H21ClN4O	1
1	IC50 = 15 nM
CP0519453 Compound Info	4-[[(3S)-piperidin-3-yl]amino]-2-thiophen-2-ylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C17H18N4OS2	1
1	IC50 = 15 nM
CP0136930 Compound Info	2-methoxy-9-(3-methoxy-4-nitrophenyl)-N,N-dimethyl-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepine-3-carboxamide Show/Hide	C24H22N4O6	1
1	IC50 = 15.5 nM
CP0035071 Compound Info	3-methoxy-9-(3-methoxy-4-nitrophenyl)-2-(2-pyridin-4-ylethyl)-5,11-dihydrobenzo[b][1,4]benzodiazepin-6-one Show/Hide	C28H24N4O5	1
1	IC50 = 16.2 nM
CP0176892 Compound Info	12-(furan-3-yl)-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C15H8N4O	1
1	IC50 = 16.6 nM
CP0045291 Compound Info	3-(Indol-2-yl)indazole 3 Show/Hide	C23H22N6O	1
1	IC50 = 17 nM
CP0552128 Compound Info	1137478-41-1 Show/Hide	C21H20FN7O	1
1	IC50 = 17 nM
CP0057267 Compound Info	methyl 6-[[5-cyano-6-[(3R)-pyrrolidin-3-yl]oxypyrazin-2-yl]amino]-4-methylsulfanylpyridine-3-carboxylate Show/Hide	C17H18N6O3S	1
1	IC50 = 18 nM
CP0153184 Compound Info	[12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl]methanol Show/Hide	C23H24N4O	1
1	IC50 = 18.3 nM
CP0251942 Compound Info	12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene Show/Hide	C22H22N4	1
1	IC50 = 18.6 nM
CP0338384 Compound Info	2-(1-benzofuran-5-yl)-N-(2-piperazin-1-ylphenyl)-1,3-thiazole-4-carboxamide Show/Hide	C22H20N4O2S	1
1	IC50 = 19 nM
CP0552173 Compound Info	methyl 6-[(5-cyanopyrazin-2-yl)amino]-4-[(1-methylpiperidin-4-yl)methylamino]pyridine-3-carboxylate Show/Hide	C19H23N7O2	1
1	IC50 = 19 nM
CP0060052 Compound Info	4-methoxy-12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene Show/Hide	C23H24N4O	1
1	IC50 = 19.8 nM
CP0083030 Compound Info	11H-2,5,11-triaza-benzo[a]trindene-1,3,4,6-tetraone Show/Hide	C16H7N3O4	1
1	IC50 = 20 nM
CP0503084 Compound Info	6-(4-hydroxy-3-methoxyphenyl)-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)quinolin-2(1H)-one Show/Hide	C30H29N3O3	1
1	IC50 = 20 nM
CP0151078 Compound Info	5-methyl-8-(thiophen-2-yl)-[1,2,4]triazolo[4,3-a]quinolin-1(2H)-one Show/Hide	C15H11N3OS	1
1	IC50 = 20 nM
CP0145930 Compound Info	5-[[5-chloro-4-(methylamino)pyridin-2-yl]amino]-3-[(2R)-1-(dimethylamino)propan-2-yl]oxypyrazine-2-carbonitrile Show/Hide	C16H20ClN7O	1
1	IC50 = 20 nM
CP0300583 Compound Info	4-[[(3S)-piperidin-3-yl]amino]-2-(1H-pyrazol-4-yl)thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C16H18N6OS	1
1	IC50 = 20 nM
CP0407788 Compound Info	12-thiophen-2-yl-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C15H8N4S	1
1	IC50 = 20.2 nM
CP0087831 Compound Info	3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[4-(methylamino)-5-(trifluoromethyl)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C17H20F3N7O	1
1	IC50 = 21 nM
CP0145934 Compound Info	methyl 6-[(5-cyanopyrazin-2-yl)amino]-4-(piperidin-4-ylmethylamino)pyridine-3-carboxylate Show/Hide	C18H21N7O2	2
1	IC50 = 21 nM
2	IC50 = 36 nM
CP0364838 Compound Info	4-[[(3S,6R)-6-methylpiperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C20H22N4OS	1
1	IC50 = 21 nM
CP0256902 Compound Info	methyl 3-[3-methoxy-9-(3-methoxy-4-nitrophenyl)-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepin-2-yl]propanoate Show/Hide	C25H23N3O7	1
1	IC50 = 22 nM
CP0558618 Compound Info	2-(4-fluorophenyl)-4-[[(3S)-piperidin-3-yl]amino]-1H-indole-7-carboxamide Show/Hide	C20H21FN4O	1
1	IC50 = 23 nM
CP0572926 Compound Info	5-[[5-cyano-4-(morpholin-2-ylmethylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C16H16N8O	1
1	IC50 = 23 nM
CP0507048 Compound Info	2-imidazol-1-yl-4-[[(3S)-piperidin-3-yl]amino]thieno[3,2-c]pyridine-7-carboxamide Show/Hide	C16H18N6OS	1
1	IC50 = 24 nM
CP0558613 Compound Info	4-[methyl-[(3S)-piperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C20H22N4OS	1
1	IC50 = 25 nM
CP0477873 Compound Info	1137478-44-4 Show/Hide	C21H20FN7O	1
1	IC50 = 25 nM
CP0087829 Compound Info	5-[[5-cyclopropyl-4-(methylamino)pyridin-2-yl]amino]-3-[(2R)-1-(dimethylamino)propan-2-yl]oxypyrazine-2-carbonitrile Show/Hide	C19H25N7O	1
1	IC50 = 26 nM
CP0276514 Compound Info	3-(1H-indol-2-yl)-6-(1H-1,2,3,4-tetrazol-5-yl)-1H-indazole Show/Hide	C16H11N7	1
1	IC50 = 27 nM
CP0169777 Compound Info	3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[5-(1-methylpyrazol-4-yl)-4-methylsulfanylpyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C20H24N8OS	1
1	IC50 = 27 nM
CP0185514 Compound Info	12-[3-(hydroxymethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C18H12N4O	1
1	IC50 = 27.1 nM
CP0338423 Compound Info	6-(3-hydroxyphenyl)-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)quinolin-2(1H)-one Show/Hide	C29H27N3O2	1
1	IC50 = 29 nM
CP0214763 Compound Info	2-phenyl-4-[[(3S)-piperidin-3-yl]amino]-1H-indole-7-carboxamide Show/Hide	C20H22N4O	1
1	IC50 = 31 nM
CP0188200 Compound Info	12-(1-methylpyrazol-3-yl)-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C15H10N6	1
1	IC50 = 33.8 nM
CP0543081 Compound Info	4-[ethyl-[(3S)-piperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C21H24N4OS	1
1	IC50 = 35 nM
CP0265689 Compound Info	3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[5-(3-fluorophenyl)-4-(methylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C22H24FN7O	1
1	IC50 = 36 nM
CP0153181 Compound Info	12-hydroxy-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C11H6N4O	1
1	IC50 = 38.1 nM
CP0109176 Compound Info	12-(2-hydroxyphenyl)-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C17H10N4O	1
1	IC50 = 41.7 nM
CP0273691 Compound Info	12-pyridin-4-yl-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C16H9N5	1
1	IC50 = 42.7 nM
CP0146141 Compound Info	methyl 6-[[5-cyano-6-[(3R)-pyrrolidin-3-yl]oxypyrazin-2-yl]amino]-4-methoxypyridine-3-carboxylate Show/Hide	C17H18N6O4	1
1	IC50 = 46.5 nM
CP0240736 Compound Info	5-[[5-phenyl-4-(piperidin-4-ylmethylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C22H23N7	1
1	IC50 = 50 nM
CP0564317 Compound Info	5-[[5-(3-hydroxypropyl)-4-(piperidin-4-ylmethylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C19H25N7O	1
1	IC50 = 54 nM
CP0552129 Compound Info	6-[(5-cyanopyrazin-2-yl)amino]-N-phenyl-4-(piperidin-4-ylmethylamino)pyridine-3-carboxamide Show/Hide	C23H24N8O	1
1	IC50 = 55 nM
CP0463932 Compound Info	2-phenyl-4-piperidin-3-ylsulfanylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C19H19N3OS2	1
1	IC50 = 56 nM
CP0477872 Compound Info	methyl 6-[(5-cyanopyrazin-2-yl)amino]-4-(piperidin-3-ylmethylamino)pyridine-3-carboxylate Show/Hide	C18H21N7O2	1
1	IC50 = 56 nM
CP0185517 Compound Info	12-(ethylamino)-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C13H11N5	1
1	IC50 = 56.6 nM
CP0507047 Compound Info	4-[[(2S,3S)-2-methylpiperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C20H22N4OS	1
1	IC50 = 69 nM
CP0003092 Compound Info	2-(2,3-dihydro-1-benzofuran-5-yl)-N-(2-piperazin-1-ylphenyl)-1,3-thiazole-4-carboxamide Show/Hide	C22H22N4O2S	2
1	IC50 = 75 nM
2	Kd < 100 nM
CP0125384 Compound Info	12-pyridin-3-yl-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C16H9N5	1
1	IC50 = 76.5 nM
CP0356195 Compound Info	12-(4-morpholin-4-ylphenyl)-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C21H17N5O	1
1	IC50 = 78.7 nM
CP0120980 Compound Info	4-[2-hydroxyethyl-[(3S)-piperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C21H24N4O2S	1
1	IC50 = 79 nM
CP0021175 Compound Info	1,11-dihydro-1,3,5,11-tetraaza-benzo[a]trindene-4,6-dione Show/Hide	C15H8N4O2	3
1	IC50 = 80 nM
2	IC50 = 81 nM
3	IC50 = 250 nM
CP0534744 Compound Info	4-[[(2R,3S)-2-(2-hydroxyethyl)piperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C21H24N4O2S	1
1	IC50 = 83 nM
CP0538857 Compound Info	2-phenyl-4-[(3S)-piperidin-3-yl]oxythieno[3,2-c]pyridine-7-carboxamide Show/Hide	C19H19N3O2S	1
1	IC50 = 83 nM
CP0570862 Compound Info	5-[[5-(3-methyl-1,2,4-oxadiazol-5-yl)-4-(piperidin-4-ylmethylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C19H21N9O	1
1	IC50 = 92 nM
CP0256603 Compound Info	3-[(2R)-1-(dimethylamino)propan-2-yl]oxy-5-[[4-(methylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C16H21N7O	1
1	IC50 = 97 nM
CP0016545 Compound Info	11H-2,5,11,11b-Tetraaza-benzo[a]trindene-4,6-dione Show/Hide	C15H8N4O2	2
1	IC50 = 100 nM
2	IC50 = 440 nM
CP0176858 Compound Info	N-ethyl-12-[4-(piperidin-1-ylmethyl)phenyl]-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene-4-carboxamide Show/Hide	C25H27N5O	1
1	IC50 = 102 nM
CP0125386 Compound Info	12-pyridin-2-yl-5,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene-4-carbonitrile Show/Hide	C16H9N5	1
1	IC50 = 127 nM
CP0414040 Compound Info	4-[[(3S)-1-methylpiperidin-3-yl]amino]-2-phenylthieno[3,2-c]pyridine-7-carboxamide Show/Hide	C20H22N4OS	1
1	IC50 = 140 nM
CP0279582 Compound Info	3-[(2S)-1-(dimethylamino)propan-2-yl]oxy-5-[[4-(methylamino)-5-(1-methylpyrazol-4-yl)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C20H25N9O	1
1	IC50 = 169 nM
CP0572925 Compound Info	5-[[5-(3-fluorophenyl)-4-(piperidin-4-ylmethylamino)pyridin-2-yl]amino]pyrazine-2-carbonitrile Show/Hide	C22H22FN7	1
1	IC50 = 177 nM
CP0684598 Compound Info	benzo[a]pyrrolo[3,4-c]carbazole-1,3,4,7(2H,8H)-tetraone Show/Hide	C18H8N2O4	1
1	IC50 = 269 nM
CP0144722 Compound Info	4,7-dihydroxybenzo[a]pyrrolo[3,4-c]carbazole-1,3(2H,8H)-dione Show/Hide	C18H10N2O4	1
1	IC50 = 311 nM
CP0519450 Compound Info	2-phenyl-4-[[(3S)-piperidin-3-yl]amino]furo[3,2-c]pyridine-7-carboxamide Show/Hide	C19H20N4O2	1
1	IC50 = 330 nM
CP0295930 Compound Info	4-(6-(morpholinomethyl)-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)benzoic acid Show/Hide	C22H21N3O3	1
1	Ki = 7.943 nM

Clinical Information about the Protein

Target 1 ( Checkpoint kinase-1 (CHK1) )

Target Type	Clinical trial Target
Disease	7 Target-related Diseases				7
1	Pancreatic cancer [ICD-11: 2C10]
2	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3	Non-small-cell lung cancer [ICD-11: 2C25.Y]
4	Ovarian cancer [ICD-11: 2C73]
5	Hodgkin lymphoma [ICD-11: 2B30]
6	Advanced solid tumour [ICD-11: 2A00-2F9Z]
7	Triple negative breast cancer [ICD-11: 2C60-2C65]
Clinical Trial Drug(s)	6 Clinical Trial Drugs				6
1	LY2603618	Drug Info	Phase 2	Pancreatic cancer
2	SCH-900776	Drug Info	Phase 2	Solid tumour/cancer
3	UCN-01	Drug Info	Phase 2	Non-small-cell lung cancer
4	AZD7762	Drug Info	Phase 1	Solid tumour/cancer
5	LY2606368	Drug Info	Phase 2	Ovarian cancer
6	MK-8776	Drug Info	Phase 1	Hodgkin lymphoma
Discontinued Drug(s)	1 Discontinued Drug				1
1	PF-477736	Drug Info	Discontinued in Phase 1	Advanced solid tumour
Investigative Drug(s)	1 Investigative Drug				1
1	SB218078	Drug Info	Investigative	Triple negative breast cancer

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han