General Information of the Protein
Protein ID
PT00934
Protein Name
High affinity nerve growth factor receptor
Secondarily
Protein Name
Neurotrophic tyrosine kinase receptor type 1
TRK1-transforming tyrosine kinase protein
Tropomyosin-related kinase A
Tyrosine kinase receptor
Tyrosine kinase receptor A
gp140trk
p140-TrkA
Gene Name
NTRK1
Secondarily
Gene Name
MTC
TRK
TRKA
Sequence
MLRGGRRGQLGWHSWAAGPGSLLAWLILASAGAAPCPDACCPHGSSGLRCTRDGALDSLHHLPGAENLTELYIENQQHLQHLELRDLRGLGELRNLTIVKSGLRFVAPDAFHFTPRLSRLNLSFNALESLSWKTVQGLSLQELVLSGNPLHCSCALRWLQRWEEEGLGGVPEQKLQCHGQGPLAHMPNASCGVPTLKVQVPNASVDVGDDVLLRCQVEGRGLEQAGWILTELEQSATVMKSGGLPSLGLTLANVTSDLNRKNVTCWAENDVGRAEVSVQVNVSFPASVQLHTAVEMHHWCIPFSVDGQPAPSLRWLFNGSVLNETSFIFTEFLEPAANETVRHGCLRLNQPTHVNNGNYTLLAANPFGQASASIMAAFMDNPFEFNPEDPIPVSFSPVDTNSTSGDPVEKKDETPFGVSVAVGLAVFACLFLSTLLLVLNKCGRRNKFGINRPAVLAPEDGLAMSLHFMTLGGSSLSPTEGKGSGLQGHIIENPQYFSDACVHHIKRRDIVLKWELGEGAFGKVFLAECHNLLPEQDKMLVAVKALKEASESARQDFQREAELLTMLQHQHIVRFFGVCTEGRPLLMVFEYMRHGDLNRFLRSHGPDAKLLAGGEDVAPGPLGLGQLLAVASQVAAGMVYLAGLHFVHRDLATRNCLVGQGLVVKIGDFGMSRDIYSTDYYRVGGRTMLPIRWMPPESILYRKFTTESDVWSFGVVLWEIFTYGKQPWYQLSNTEAIDCITQGRELERPRACPPEVYAIMRGCWQREPQQRHSIKDVHARLQALAQAPPVYLDVLG
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Trk family
Function
Receptor tyrosine kinase involved in the development and the maturation of the central and peripheral nervous systems through regulation of proliferation, differentiation and survival of sympathetic and nervous neurons. High affinity receptor for NGF which is its primary ligand (PubMed:1850821, PubMed:1849459, PubMed:1281417, PubMed:8325889, PubMed:15488758, PubMed:22649032, PubMed:17196528, PubMed:27445338). Can also bind and be activated by NTF3/neurotrophin-3. However, NTF3 only supports axonal extension through NTRK1 but has no effect on neuron survival (By similarity). Upon dimeric NGF ligand-binding, undergoes homodimerization, autophosphorylation and activation (PubMed:1281417). Recruits, phosphorylates and/or activates several downstream effectors including SHC1, FRS2, SH2B1, SH2B2 and PLCG1 that regulate distinct overlapping signaling cascades driving cell survival and differentiation. Through SHC1 and FRS2 activates a GRB2-Ras-MAPK cascade that regulates cell differentiation and survival. Through PLCG1 controls NF-Kappa-B activation and the transcription of genes involved in cell survival. Through SHC1 and SH2B1 controls a Ras-PI3 kinase-AKT1 signaling cascade that is also regulating survival. In absence of ligand and activation, may promote cell death, making the survival of neurons dependent on trophic factors.
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Uniprot ID
Primary ID:
P04629

Secondarily ID:
B2R6T5
B7ZM34
P08119
Q15655
Q15656
Q5D056
Q5VZS2
Q7Z5C3
Q9UIU7
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Ensembl ID
ENSG00000198400
HGNC ID
HGNC:8031
Subcellular Location
Cell membrane
Early endosome membrane
Late endosome membrane
Recycling endosome membrane
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: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0137907
2-(4-methylpiperazin-1-yl)-N-[4-methyl-5-[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]-1,3-thiazol-2-yl]acetamide
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C25H27N7OS
 7
1
EC50 = 26 nM
   TI
   LI
   LO
   TS
2
EC50 = 67 nM
   TI
   LI
   LO
   TS
3
EC50 = 120 nM
   TI
   LI
   LO
   TS
4
GI50 = 7 nM
   TI
   LI
   LO
   TS
5
GI50 = 8.5 nM
   TI
   LI
   LO
   TS
6
GI50 = 34 nM
   TI
   LI
   LO
   TS
7
GI50 = 194 nM
   TI
   LI
   LO
   TS
CP0870202
N-{4-Methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-2-(3-trifluoromethyl-phenyl)-acetamide
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C27H20F3N5OS
 1
1
GI50 = 2 nM
   TI
   LI
   LO
   TS
CP0966460
2-(3-Chloro-phenyl)-N-{4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-acetamide
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C26H20ClN5OS
 1
1
GI50 = 2 nM
   TI
   LI
   LO
   TS
CP0946572
1-{4-Methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-3-(3-trifluoromethyl-phenyl)-urea
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C26H19F3N6OS
 1
1
GI50 = 3 nM
   TI
   LI
   LO
   TS
CP0963126
N-{4-Methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-3-trifluoromethyl-benzamide
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C26H18F3N5OS
 1
1
GI50 = 3 nM
   TI
   LI
   LO
   TS
CP0910645
Selitrectinib
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C20H21FN6O
 3
1
GI50 = 5 nM
   TI
   LI
   LO
   TS
2
GI50 = 6 nM
   TI
   LI
   LO
   TS
3
GI50 = 10 nM
   TI
   LI
   LO
   TS
CP0964277
4-(4-Methyl-piperazin-1-ylmethyl)-N-{4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-benzamide
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C31H31N7OS
 1
1
GI50 = 8 nM
   TI
   LI
   LO
   TS
CP0898527
2-Amino-N-{4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-4-methylsulfanyl-butyramide
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C23H24N6OS2
 1
1
GI50 = 13 nM
   TI
   LI
   LO
   TS
CP0911397
(E)-N-(4((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-4-yl)vinyl)-1H-indazol-6-yl)thio)propanamide
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C30H31F3N6OS
 1
1
GI50 = 18 nM
   TI
   LI
   LO
   TS
CP0911398
2-[4-(2-Hydroxy-ethyl)-piperazin-1-yl]-N-{4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-acetamide
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C26H29N7O2S
 1
1
GI50 = 18 nM
   TI
   LI
   LO
   TS
CP0257372
US10005783, 14
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C21H22F2N6O2
 3
1
GI50 = 29 nM
   TI
   LI
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2
GI50 = 602 nM
   TI
   LI
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3
GI50 = 1190 nM
   TI
   LI
   LO
   TS
CP0898533
2-(1-Methyl-piperidin-4-yl)-N-{4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-acetamide
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C26H28N6OS
 1
1
GI50 = 32 nM
   TI
   LI
   LO
   TS
CP0910644
N-{4-Methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-2-naphthalen-1-yl-acetamide
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C30H23N5OS
 1
1
GI50 = 33 nM
   TI
   LI
   LO
   TS
CP0946569
2-(2-Methoxy-ethoxy)-N-{4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-acetamide
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C23H23N5O3S
 1
1
GI50 = 35 nM
   TI
   LI
   LO
   TS
CP0946568
2-(3,4-Dimethoxy-phenyl)-N-{4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-acetamide
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C28H25N5O3S
 1
1
GI50 = 40 nM
   TI
   LI
   LO
   TS
CP0946567
4-(4-Methyl-piperazin-1-ylmethyl)-N-{4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-thiazol-2-yl}-3-trifluoromethyl-benzamide
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C32H30F3N7OS2
 1
1
GI50 = 44 nM
   TI
   LI
   LO
   TS
CP0898529
N-{5-[3-(5-Fluoro-pyridin-3-yl)-1H-indazol-6-yl]-4-methyl-thiazol-2-yl}-2-(4-methyl-piperazin-1-yl)-acetamide
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C23H24FN7OS
 1
1
GI50 = 54 nM
   TI
   LI
   LO
   TS
CP0946566
1-[4-(4-Methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-3-{3-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-phenyl}-urea
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C34H32F3N7OS
 1
1
GI50 = 62 nM
   TI
   LI
   LO
   TS
CP0441015
N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]propanamide
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C30H31F3N6OS
 1
1
GI50 = 63 nM
   TI
   LI
   LO
   TS
CP0964883
2-Amino-N-{4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-3-phenyl-propionamide
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C27H24N6OS
 1
1
GI50 = 68 nM
   TI
   LI
   LO
   TS
CP0898530
N-{4-Methyl-5-[3-(1-methyl-1H-pyrazol-3-yl)-1H-indazol-6-yl]-thiazol-2-yl}-2-(4-methyl-piperazin-1-yl)-acetamide
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C22H26N8OS
 1
1
GI50 = 73 nM
   TI
   LI
   LO
   TS
CP0964873
N-[4-(4-Methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-3-[3-((E)-2-pyrazin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-propionamide
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C29H30F3N7OS
 1
1
GI50 = 88 nM
   TI
   LI
   LO
   TS
CP0911399
1-Methyl-piperidine-4-carboxylic acid {4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-amide
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C25H26N6OS
 1
1
GI50 = 89 nM
   TI
   LI
   LO
   TS
CP0869891
N-{4-Methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-2-piperidin-4-yl-acetamide
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C25H26N6OS
 1
1
GI50 = 116 nM
   TI
   LI
   LO
   TS
CP0898528
Piperidine-4-carboxylic acid {4-methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-amide
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C24H24N6OS
 1
1
GI50 = 145 nM
   TI
   LI
   LO
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CP0870201
N-[4-(4-Methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-N'-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-malonamide
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C30H30F3N7O2
 1
1
GI50 = 248 nM
   TI
   LI
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CP0870207
N-(4-methyl-5-(3-(pyridin-3-yl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide
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C23H25N7OS
 1
1
GI50 = 251 nM
   TI
   LI
   LO
   TS
CP0946571
N-{4-Methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-isobutyramide
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C22H21N5OS
 1
1
GI50 = 251 nM
   TI
   LI
   LO
   TS
CP0870205
N-{4-Methyl-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-yl]-thiazol-2-yl}-2-piperidin-3-yl-acetamide
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C25H26N6OS
 1
1
GI50 = 300 nM
   TI
   LI
   LO
   TS
CP0898532
(E)-4-((4-Methylpiperazin-1-yl)methyl)-N-(2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)ethyl)-3-(trifluoromethyl)benzamide
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C30H31F3N6OS
 1
1
GI50 = 370 nM
   TI
   LI
   LO
   TS
CP0928211
(E)-4-((4-Methylpiperazin-1-yl)methyl)-N-(3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propyl)-3-(trifluoromethyl)benzamide
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C31H33F3N6OS
 1
1
GI50 = 370 nM
   TI
   LI
   LO
   TS
CP0910643
N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(pyridin-4-yl)-1H-indazol-6-yl)thio)propanamide
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C28H29F3N6OS
 1
1
GI50 = 448 nM
   TI
   LI
   LO
   TS
CP0898531
N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(6-methylpyridin-3-yl)-1H-indazol-6-yl)thio)propanamide
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C29H31F3N6OS
 1
1
GI50 = 516 nM
   TI
   LI
   LO
   TS
CP0946570
(E)-1-(4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)ethyl)urea
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C30H32F3N7OS
 1
1
GI50 = 646 nM
   TI
   LI
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CP0964878
3-((3-Methyl-1H-indazol-6-yl)thio)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)propanamide
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C24H28F3N5OS
 1
1
GI50 = 729 nM
   TI
   LI
   LO
   TS
CP0962729
N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(pyridin-3-yl)-1H-indazol-6-yl)thio)propanamide
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C28H29F3N6OS
 1
1
GI50 = 736 nM
   TI
   LI
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   TS
CP0961918
N-{5-[3-(2-Amino-pyrimidin-5-yl)-1H-indazol-6-yl]-4-methyl-thiazol-2-yl}-2-(4-methyl-piperazin-1-yl)-acetamide
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C22H25N9OS
 1
1
GI50 = 752 nM
   TI
   LI
   LO
   TS
CP0869913
4-(4-Methyl-piperazin-1-ylmethyl)-N-{3-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylsulfanyl]-phenyl}-3-trifluoromethyl-benzamide
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C34H31F3N6OS
 1
1
GI50 = 920 nM
   TI
   LI
   LO
   TS
CP0965397
N-{5-[3-(3-Fluoro-phenyl)-1H-indazol-6-yl]-4-methyl-thiazol-2-yl}-2-(4-methyl-piperazin-1-yl)-acetamide
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C24H25FN6OS
 1
1
GI50 = 1490 nM
   TI
   LI
   LO
   TS
CP0898526
(E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)acetamide
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C20H17N5OS
 1
1
GI50 = 4310 nM
   TI
   LI
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   TS
CP0385508
2-[4-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acid
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C27H28FN7O2
 1
1
IC50 = 1 nM
   TI
   LI
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   TS
CP0395047
6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]-3-pyridin-2-ylimidazo[1,2-b]pyridazine
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C21H18FN5
 1
1
IC50 = 3 nM
   TI
   LI
   LO
   TS
CP0385511
1-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol
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C26H27FN6O
 2
1
IC50 = 3 nM
   TI
   LI
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   TS
2
IC50 = 4 nM
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   LI
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CP0546748
5,18-dimethyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-14-oxo-9-oxa-15,18,23,25,26-pentazatetracyclo[17.5.2.14,8.022,25]heptacosa-1(24),4,6,8(27),19(26),20,22-heptaen-2-yne-6-carboxamide
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C35H33F3N8O3
 3
1
IC50 = 3.1 nM
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2
IC50 = 12.5 nM
   TI
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3
IC50 = 50 nM
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CP0433699
1-[6-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol
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C26H27FN6O
 1
1
IC50 = 5 nM
   TI
   LI
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   TS
CP0859348
N-[3-(6-{[(3-Fluorophenyl)methyl]amino}imidazo[1,2-b]pyridazin-3-yl)phenyl]oxane-4-carboxamide
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C25H24FN5O2
 1
1
IC50 = 6 nM
   TI
   LI
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   TS
CP0433700
4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C23H18FN5
 1
1
IC50 = 21 nM
   TI
   LI
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   TS
CP0543110
4-[6-[(3-fluorophenyl)methylamino]imidazo[1,2-b]pyridazin-3-yl]benzenesulfonamide
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C19H16FN5O2S
 1
1
IC50 = 27 nM
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   TS
CP0488257
4-[6-[(3-fluorophenyl)methylamino]imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C20H14FN5
 1
1
IC50 = 50 nM
   TI
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CP0530865
4-[6-[2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C23H18FN5
 1
1
IC50 = 68 nM
   TI
   LI
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CP0542684
4-[6-[3-(3-fluorophenyl)morpholin-4-yl]imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C23H18FN5O
 1
1
IC50 = 75 nM
   TI
   LI
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   TS
CP0510927
[4-[6-[(3-fluorophenyl)methylamino]imidazo[1,2-b]pyridazin-3-yl]phenyl]methanol
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C20H17FN4O
 1
1
IC50 = 76 nM
   TI
   LI
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CP0561248
4-[6-[2-(3-fluorophenyl)piperidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]benzonitrile
   Show/Hide
C24H20FN5
 1
1
IC50 = 170 nM
   TI
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   TS
CP0856137
4-(6-{[(2-Methoxyphenyl)methyl]amino}imidazo[1,2-b]pyridazin-3-yl)benzonitrile
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C21H17N5O
 1
1
IC50 = 170 nM
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CP0510926
4-[6-[benzyl(methyl)amino]imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C21H17N5
 1
1
IC50 = 520 nM
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CP0922172
3-[6-(Benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C20H15N5
 1
1
IC50 = 740 nM
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CP0388864
4-[6-(benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C20H15N5
 1
1
IC50 = 850 nM
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CP0061016
3-(4-Amino-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-phenol
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C17H18N4O
 1
1
IC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0418567
3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol
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C17H18N4O2
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0388620
methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
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C28H32N6O5
 1
1
IC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0395369
4-[6-[(2S)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C23H18FN5
 1
1
IC50 = 3130 nM
   TI
   LI
   LO
   TS
CP0138866
1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone
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C22H25FN6O2
 1
1
IC50 = 9300 nM
   TI
   LI
   LO
   TS
CP0388615
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine
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C23H26N6O3S
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
CP0388616
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine
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C26H29N5O3
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0203683
1-propan-2-yl-1-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-3-[4-(trifluoromethoxy)phenyl]urea
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C19H19F3N4O2
 2
1 EC50 = 11.3 nM
2 IC50 = 11 nM
CP0115354
1-propan-2-yl-1-[[3-(1,3-thiazol-2-yl)phenyl]methyl]-3-[4-(trifluoromethoxy)phenyl]urea
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C21H20F3N3O2S
 3
1 EC50 = 119 nM
2 IC50 = 132 nM
3 Kd = 63 nM
CP0354714
Loxo-195
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C20H21FN6O
 16
1 IC50 = 0.07 nM
2 IC50 = 0.98 nM
3 IC50 < 1 nM
4 IC50 = 2 nM
5 IC50 = 2.1 nM
6 IC50 = 3.7 nM
7 IC50 = 5.5 nM
8 IC50 = 5.8 nM
9 IC50 = 6.2 nM
10 IC50 = 6.7 nM
11 IC50 = 7.6 nM
12 IC50 = 9.3 nM
13 IC50 = 9.8 nM
14 IC50 = 12.6 nM
15 IC50 = 110 nM
16 IC50 = 300 nM
CP0257372
US10005783, 14
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C21H22F2N6O2
 20
1 IC50 = 0.4 nM
2 IC50 = 1.2 nM
3 IC50 = 1.31 nM
4 IC50 = 1.96 nM
5 IC50 = 2 nM
6 IC50 = 2.9 nM
7 IC50 = 5 nM
8 IC50 = 5.6 nM
9 IC50 = 6.5 nM
10 IC50 = 9.7 nM
11 IC50 = 32.2 nM
12 IC50 = 38.6 nM
13 IC50 = 43.1 nM
14 IC50 = 45 nM
15 IC50 = 69 nM
16 IC50 = 109.4 nM
17 IC50 = 140 nM
18 IC50 = 237.4 nM
19 IC50 = 272 nM
20 IC50 = 1214 nM
CP0035306
2-amino-1-(4-(5-(2-(6-bromopyridin-2-ylamino)thiazol-5-ylthio)-2-methylbenzoyl)piperazin-1-yl)ethanone
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C22H23BrN6O2S2
 1
1 IC50 = 0.6 nM
CP0186372
5-(carbamoylamino)-3-[(5R)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ylsulfanyl]-1,2-thiazole-4-carboxamide
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C16H18N4O2S2
 1
1 IC50 < 1 nM
CP0186373
5-(carbamoylamino)-3-{6,7,8,9-tetrahydro-5H-benzo[7]annulen-5-ylsulfanyl}-1,2-thiazole-4-carboxamide
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C16H18N4O2S2
 1
1 IC50 < 1 nM
CP0020453
US10081622, Compound 11
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C31H34F2N6O2
 3
1 IC50 = 1 nM
2 IC50 = 1.7 nM
3 IC50 < 10 nM
CP0161876
methyl (15S,16S,18R)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate
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C27H21N3O5
 1
1 IC50 = 1.2 nM
CP0273324
N-tert-butyl-2-[2-[8-(methanesulfonamido)-6,6-dimethyl-11-oxonaphtho[2,3-b][1]benzofuran-3-yl]ethynyl]-6-methylpyridine-4-carboxamide
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C32H31N3O5S
 2
1 IC50 = 1.2 nM
2 IC50 = 3000 nM
CP0026342
3-((1-methyl-1H-indol-3-yl)methylene)-1H-pyrrolo[3,2-b]pyridin-2(3H)-one
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C17H13N3O
 1
1 IC50 = 2 nM
CP0836005
LAROTRECTINIB SULFATE
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C21H24F2N6O6S
 2
1 IC50 = 2 nM
2 IC50 = 5 nM
CP0579359
5,18-dimethyl-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-14-oxo-9-oxa-15,18,23,25,26-pentazatetracyclo[17.5.2.14,8.022,25]heptacosa-1(24),4,6,8(27),19(26),20,22-heptaen-2-yne-6-carboxamide
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C37H41F3N8O3
 2
1 IC50 = 2.7 nM
2 IC50 = 80.6 nM
CP0136781
3-{[1-(4-chlorophenyl)ethyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamide
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C14H15ClN4O2S2
 1
1 IC50 = 3 nM
CP0051743
(15S,16S,18R)-16-hydroxy-15,16-dimethyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one
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C26H21N3O3
 1
1 IC50 = 3 nM
CP0284251
US8846698, 250
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C23H21ClN6O2
 1
1 IC50 = 3.48 nM
CP0130033
3-[1-(5-Methoxy-1-methyl-1H-indol-3-yl)-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid methylamide
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C20H19N3O4S
 1
1 IC50 = 3.66 nM
CP0053535
3-[1-(5-Methoxy-1-methyl-1H-indol-3-yl)-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid amide
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C19H17N3O4S
 1
1 IC50 = 3.78 nM
CP0533869
1-[[5-(methoxymethyl)-2-(trifluoromethoxy)phenyl]methyl]-3-(8-methyl-2-phenylimidazo[1,2-a]pyrazin-3-yl)urea
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C24H22F3N5O3
 2
1 IC50 = 3.9 nM
2 IC50 = 10.97 nM
CP0559176
(3R)-N-[5-[(2S)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxypyrrolidine-1-carboxamide
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C21H22F2N6O2
 1
1 IC50 = 3.9 nM
CP0514699
US8846698, 253
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C23H24N8O2
 1
1 IC50 = 3.92 nM
CP0285447
3-{[(1R)-1-(4-chlorophenyl)propyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamide
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C15H17ClN4O2S2
 1
1 IC50 = 4 nM
CP0016242
3-((1-methyl-1H-indol-3-yl)methylene)-2-oxoindoline-5-sulfonamide
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C18H15N3O3S
 1
1 IC50 = 4.17 nM
CP0025712
3-(5-Hydroxy-indan-1-ylidene)-1,3-dihydro-indol-2-one
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C17H13NO2
 1
1 IC50 = 6 nM
CP0639664
GW278681X
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C16H15N3O3S
 1
1 IC50 = 6 nM
CP0546748
5,18-dimethyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-14-oxo-9-oxa-15,18,23,25,26-pentazatetracyclo[17.5.2.14,8.022,25]heptacosa-1(24),4,6,8(27),19(26),20,22-heptaen-2-yne-6-carboxamide
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C35H33F3N8O3
 2
1 IC50 = 6.17 nM
2 IC50 = 493.7 nM
CP0297089
3-{[(4-chlorophenyl)methyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamide
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C13H13ClN4O2S2
 1
1 IC50 = 7 nM
CP0641705
GW284408X
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C16H12N4O2
 1
1 IC50 = 7 nM
CP0045140
3-[(5-chloro-2,3-dihydro-1H-inden-1-yl)sulfanyl]-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamide
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C15H15ClN4O2S2
 1
1 IC50 = 8 nM
CP0022559
5-Bromo-3-(5-bromo-6-hydroxy-2'-methoxy-biphenyl-3-ylmethylene)-1,3-dihydro-pyrrolo[2,3-b]pyridin-2-one
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C21H14Br2N2O3
 1
1 IC50 = 8 nM
CP0639797
GW301789X
   Show/Hide
C17H13N5O
 1
1 IC50 = 8 nM
CP0367394
US8846698, 90
   Show/Hide
C23H23N7O2
 1
1 IC50 = 8.81 nM
CP0109923
3-{[1-(4-chlorophenyl)propyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamide
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C15H17ClN4O2S2
 1
1 IC50 = 9 nM
CP0007238
Oxindole (Scaffold V)
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C21H15N5O3S2
 1
1 IC50 = 9 nM
CP0156003
N-(5-tert-butyl-2-pyridin-3-ylpyrazol-3-yl)-2-[4-(6-imidazol-1-ylpyridin-3-yl)triazol-1-yl]acetamide
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C24H24N10O
 2
1 IC50 = 9 nM
2 Kd = 0.94 nM
CP0501115
5-(carbamoylamino)-3-[(5-chloro-2,3-dihydro-1H-inden-1-yl)sulfanyl]-1,2-thiazole-4-carboxamide
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C14H13ClN4O2S2
 1
1 IC50 = 10 nM
CP0130019
3-[1-(5-Methoxy-1-methyl-1H-indol-3-yl)-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid dimethylamide
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C21H21N3O4S
 1
1 IC50 = 10.09 nM
CP0137907
2-(4-methylpiperazin-1-yl)-N-[4-methyl-5-[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]-1,3-thiazol-2-yl]acetamide
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C25H27N7OS
 1
1 IC50 = 10.5 nM
CP0188940
US8846698, 69
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C23H20ClN5O2
 1
1 IC50 = 10.9 nM
CP0015745
3-(1-Methyl-1H-indol-3-ylmethylene)-1,3-dihydro-pyrrolo[2,3-b]pyridin-2-one
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C17H13N3O
 1
1 IC50 = 12 nM
CP0024455
5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide
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C26H32N6O2
 1
1 IC50 = 15 nM
CP0502050
3-{[1-(4-chlorophenyl)-2-methylpropyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamide
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C16H19ClN4O2S2
 1
1 IC50 = 16 nM
CP0110136
3-{[(4-chlorophenyl)methyl]sulfanyl}-5-(pyridin-3-ylamino)-1,2-thiazole-4-carboxamide
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C16H13ClN4OS2
 1
1 IC50 = 19 nM
CP0142175
US9163021, 90
   Show/Hide
C24H23FN6O2
 1
1 IC50 = 19.6 nM
CP0129156
US9242977, 85-117
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C24H20ClF3N6O2S
 1
1 IC50 = 20 nM
CP0302038
US9242977, 66-19
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C33H32N8O4S
 1
1 IC50 = 20 nM
CP0542800
1-[4-[2-[(7-ethoxy-6-fluoroquinazolin-4-yl)amino]ethyl]phenyl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]urea
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C27H25F4N5O3
 1
1 IC50 = 21.4 nM
CP0579493
3-[2-[6-[(3S)-3-aminopiperidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]ethynyl]-N-[3-chloro-5-(trifluoromethyl)phenyl]-2-methylbenzamide
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C28H24ClF3N6O
 2
1 IC50 = 22.2 nM
2 IC50 = 2608 nM
CP0580230
(6S)-N-[3-chloro-5-(trifluoromethyl)phenyl]-18-methyl-8-oxo-13-oxa-2,7,14,24,28,29-hexazapentacyclo[20.5.2.12,6.115,19.025,29]hentriaconta-1(28),15(30),16,18,22,24,26-heptaen-20-yne-17-carboxamide
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C33H31ClF3N7O3
 1
1 IC50 = 24.5 nM
CP0322061
US9163021, 21
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C22H19F3N6O2
 1
1 IC50 = 27.1 nM
CP0393683
(3Z)-3-[(5-methoxy-1H-indol-3-yl)methylidene]-1H-indol-2-one
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C18H14N2O2
 1
1 IC50 = 27.21 nM
CP0180471
5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-(2-methylsulfonylethyl)piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide
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C25H31N5O3S
 1
1 IC50 = 30 nM
CP0251769
US9242977, 57
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C31H24F3N7O3S
 1
1 IC50 = 30 nM
CP0414641
US9242977, 71
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C33H32N10O3S
 1
1 IC50 = 30 nM
CP0515510
US9242977, 72-7
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C30H26N8O3S
 1
1 IC50 = 30 nM
CP0579387
N-[3-chloro-5-(trifluoromethyl)phenyl]-5,18-dimethyl-14-oxo-9-oxa-15,18,23,25,26-pentazatetracyclo[17.5.2.14,8.022,25]heptacosa-1(24),4,6,8(27),19(26),20,22-heptaen-2-yne-6-carboxamide
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C31H28ClF3N6O3
 1
1 IC50 = 32.4 nM
CP0146125
3-{[(4-chlorophenyl)methyl]sulfanyl}-5-(pyridin-2-ylamino)-1,2-thiazole-4-carboxamide
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C16H13ClN4OS2
 1
1 IC50 = 33 nM
CP0576673
(6S)-N-[3-chloro-5-(trifluoromethyl)phenyl]-19-methyl-14-oxo-2,7,15,25,29,30-hexazapentacyclo[21.5.2.12,6.116,20.026,30]dotriaconta-1(29),16(31),17,19,23,25,27-heptaen-21-yne-18-carboxamide
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C35H35ClF3N7O2
 1
1 IC50 = 33.6 nM
CP0110138
3-{[1-(4-chlorophenyl)butyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamide
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C16H19ClN4O2S2
 1
1 IC50 = 35 nM
CP0264758
US9242977, 54
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C30H22F3N7O3S
 1
1 IC50 = 40 nM
CP0319107
US9242977, 50
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C30H20F6N8O3S
 1
1 IC50 = 40 nM
CP0340577
3-{[(4-chlorophenyl)methyl]sulfanyl}-5-(pyridin-4-ylamino)-1,2-thiazole-4-carboxamide
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C16H13ClN4OS2
 1
1 IC50 = 45 nM
CP0551990
(6S)-N-[3-chloro-5-(trifluoromethyl)phenyl]-20-methyl-15-oxo-2,7,16,26,30,31-hexazapentacyclo[22.5.2.12,6.117,21.027,31]tritriaconta-1(30),17(32),18,20,24,26,28-heptaen-22-yne-19-carboxamide
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C36H37ClF3N7O2
 1
1 IC50 = 48.1 nM
CP0228183
US9242977, 66-72
   Show/Hide
C31H31N9O5S2
 1
1 IC50 = 50 nM
CP0302039
US9242977, 72-1
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C29H23F3N8O3S
 1
1 IC50 = 50 nM
CP0221518
5-(1H-pyrazol-5-yl)-1-[2-[4-(trifluoromethoxy)phenoxy]ethyl]indole-2-carboxylic acid
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C21H16F3N3O4
 1
1 IC50 = 51 nM
CP0136779
3-{[(1S)-1-(4-chlorophenyl)propyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamide
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C15H17ClN4O2S2
 1
1 IC50 = 52 nM
CP0510522
N-(5-cyclopropyl-2-phenylpyrazol-3-yl)-2-[4-[4-(4-methylimidazol-1-yl)phenyl]triazol-1-yl]acetamide
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C26H24N8O
 1
1 IC50 = 60 nM
CP0227337
US9242977, 72-3
   Show/Hide
C30H26F2N8O3S
 1
1 IC50 = 60 nM
CP0025295
5-Bromo-3-(3-phenoxy-benzylidene)-1,3-dihydro-pyrrolo[2,3-b]pyridin-2-one
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C20H13BrN2O2
 1
1 IC50 = 61 nM
CP0117061
US9242977, 66-28
   Show/Hide
C33H33N9O4S
 1
1 IC50 = 80 nM
CP0323802
US9242977, 65-1
   Show/Hide
C33H34N8O3S
 1
1 IC50 = 80 nM
CP0326832
US9242977, 23
   Show/Hide
C29H24F3N7O2S
 1
1 IC50 = 90 nM
CP0292059
5-(carbamoylamino)-3-(1,2,3,4-tetrahydronaphthalen-1-ylsulfanyl)-1,2-thiazole-4-carboxamide
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C15H16N4O2S2
 1
1 IC50 = 105 nM
CP0323559
US9163021, 26
   Show/Hide
C24H24N6O2
 1
1 IC50 = 108 nM
CP0275029
3-{[1-(4-chlorophenyl)-2,2,2-trifluoroethyl]sulfanyl}-5-[(methylcarbamoyl)amino]-1,2-thiazole-4-carboxamide
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C14H12ClF3N4O2S2
 1
1 IC50 = 110 nM
CP0552178
5-[(methylcarbamoyl)amino]-3-(1,2,3,4-tetrahydronaphthalen-1-ylsulfanyl)-1,2-thiazole-4-carboxamide
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C16H18N4O2S2
 1
1 IC50 = 111 nM
CP0229644
5-cyano-1-[2-[4-(trifluoromethoxy)phenoxy]ethyl]indole-2-carboxylic acid
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C19H13F3N2O4
 1
1 IC50 = 118 nM
CP0319106
US9242977, 48
   Show/Hide
C28H22F3N7O3S
 1
1 IC50 = 120 nM
CP0251770
US9242977, 66-27
   Show/Hide
C33H32N8O5S
 1
1 IC50 = 130 nM
CP0317451
US8846698, 71
   Show/Hide
C24H20N6O2
 1
1 IC50 = 135 nM
CP0562354
US9242977, 9
   Show/Hide
C31H22F6N8O3S
 1
1 IC50 = 160 nM
CP0369561
3-{[(4-chlorophenyl)methyl]sulfanyl}-5-[(6-methoxypyridin-3-yl)amino]-1,2-thiazole-4-carboxamide
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C17H15ClN4O2S2
 1
1 IC50 = 179 nM
CP0107004
US9242977, 34
   Show/Hide
C31H27F3N6O2S
 1
1 IC50 = 180 nM
CP0319108
US9242977, 59
   Show/Hide
C34H30F3N7O3S
 1
1 IC50 = 190 nM
CP0233114
4-(3-ethoxyphenyl)-1-[2-[4-(trifluoromethoxy)phenoxy]ethyl]pyrrolo[3,2-c]pyridine-2-carboxylic acid
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C25H21F3N2O5
 1
1 IC50 = 348 nM
CP0580237
(6S)-N-[3-chloro-5-(trifluoromethyl)phenyl]-18-methyl-13-oxo-2,7,14,24,28,29-hexazapentacyclo[20.5.2.12,6.115,19.025,29]hentriaconta-1(28),15(30),16,18,22,24,26-heptaen-20-yne-17-carboxamide
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C34H33ClF3N7O2
 1
1 IC50 = 419 nM
CP0369564
3-[(cyclohexylmethyl)sulfanyl]-5-(pyridin-3-ylamino)-1,2-thiazole-4-carboxamide
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C16H20N4OS2
 1
1 IC50 = 610 nM
CP0064410
1-[2-(4-chlorophenoxy)ethyl]-4-(3-ethoxyphenyl)pyrrolo[3,2-c]pyridine-2-carboxylic acid
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C24H21ClN2O4
 2
1 IC50 = 653 nM
2 Kd = 3.5 nM
CP0115352
N-(5-cyclopropyl-2-phenylpyrazol-3-yl)-2-[4-[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]triazol-1-yl]acetamide
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C27H26N8O2
 2
1 IC50 = 662 nM
2 Kd = 27 nM
CP0354293
4-(3-ethoxyphenyl)-1-(2-phenoxyethyl)pyrrolo[3,2-c]pyridine-2-carboxylic acid
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C24H22N2O4
 1
1 IC50 = 2070 nM
CP0156004
1-cyclopropyl-1-[[3-(1,3-thiazol-2-yl)phenyl]methyl]-3-[4-(trifluoromethoxy)phenyl]urea
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C21H18F3N3O2S
 2
1 IC50 = 4233 nM
2 Kd = 400 nM
CP0063175
2-(2-Hydroxy-ethylamino)-5-nitro-benzo[de]isoquinoline-1,3-dione(ALE-0540)
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C14H11N3O5
 1
1 IC50 = 5880 nM
CP0156005
1-[2-[4-(trifluoromethoxy)phenoxy]ethyl]pyrrolo[3,2-c]pyridine-2-carboxylic acid
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C17H13F3N2O4
 1
1 IC50 = 12300 nM
CP0123936
2-[(3R,4S)-3-fluoro-1-[2-[4-(trifluoromethoxy)phenyl]acetyl]piperidin-4-yl]oxy-5-(1-methylimidazol-4-yl)pyridine-3-carboxamide
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C24H23F4N5O4
 1
1 Kd = 0.7 nM
CP0198981
6-amino-5-[(3S)-4,4-difluoro-1-[2-[4-(trifluoromethoxy)phenyl]acetyl]pyrrolidin-3-yl]oxy-N-methylpyridine-3-carboxamide
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C20H19F5N4O4
 1
1 Kd = 2.3 nM
CP0198982
2-[(3R,4S)-3-fluoro-1-[2-[4-(trifluoromethoxy)phenyl]acetyl]piperidin-4-yl]oxy-4-(2-hydroxy-2-methylpropoxy)benzamide
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C25H28F4N2O6
 1
1 Kd = 2.6 nM
CP0106653
5-chloro-2-N-[(1S)-1-(5-fluoropyridin-2-yl)ethyl]-4-N-(3-propan-2-yloxy-1H-pyrazol-5-yl)pyrimidine-2,4-diamine
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C17H19ClFN7O
 2
1 Ki = 0.36 nM
2 Ki = 3.7 nM
CP0230588
1-[5-[(7-methyl-4-oxopyrido[1,2-a]pyrimidin-2-yl)methylsulfanyl]-1,3,4-thiadiazol-2-yl]-3-[3-(trifluoromethyl)phenyl]urea
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C20H15F3N6O2S2
 2
1 Ki = 21 nM
2 Ki = 67 nM
Clinical Information about the Protein
Target 1 ( Tropomyosin-related kinase A (TrkA) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Non-small-cell lung cancer [ICD-11: 2C25]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved Drug(s) 3 Approved Drugs  3
1 Entrectinib Approved
Non-small-cell lung cancer
2 Repotrectinib Approved
Non-small-cell lung cancer
3 Larotrectinib Approved
Solid tumour/cancer
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 LOXO-195 Phase 1
Solid tumour/cancer
2 Altiratinib Phase 1
Solid tumour/cancer
Patented Agent(s) 1 Patented Agent  1
1 Benzimidazole derivative 6 Patented
Solid tumour/cancer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06761 High affinity nerve growth factor receptor Rattus norvegicus, Rat