General Information of the Protein
Protein ID
PT01129
Protein Name
Activin receptor type-1
Secondarily
Protein Name
Activin receptor type I
Activin receptor-like kinase 2
Serine/threonine-protein kinase receptor R1
TGF-B superfamily receptor type I
Gene Name
ACVR1
Secondarily
Gene Name
ACVRLK2
Sequence
MVDGVMILPVLIMIALPSPSMEDEKPKVNPKLYMCVCEGLSCGNEDHCEGQQCFSSLSINDGFHVYQKGCFQVYEQGKMTCKTPPSPGQAVECCQGDWCNRNITAQLPTKGKSFPGTQNFHLEVGLIILSVVFAVCLLACLLGVALRKFKRRNQERLNPRDVEYGTIEGLITTNVGDSTLADLLDHSCTSGSGSGLPFLVQRTVARQITLLECVGKGRYGEVWRGSWQGENVAVKIFSSRDEKSWFRETELYNTVMLRHENILGFIASDMTSRHSSTQLWLITHYHEMGSLYDYLQLTTLDTVSCLRIVLSIASGLAHLHIEIFGTQGKPAIAHRDLKSKNILVKKNGQCCIADLGLAVMHSQSTNQLDVGNNPRVGTKRYMAPEVLDETIQVDCFDSYKRVDIWAFGLVLWEVARRMVSNGIVEDYKPPFYDVVPNDPSFEDMRKVVCVDQQRPNIPNRWFSDPTLTSLAKLMKECWYQNPSARLTALRIKKTLTKIDNSLDKLKTDC
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TKL protein kinase group
>
TKL protein kinase STKR family
>
TKL protein kinase STKR1
Function
Bone morphogenetic protein (BMP) type I receptor that is involved in a wide variety of biological processes, including bone, heart, cartilage, nervous, and reproductive system development and regulation (PubMed:20628059, PubMed:22977237). As a type I receptor, forms heterotetrameric receptor complexes with the type II receptors AMHR2, ACVR2A or ACVR2B (PubMed:17911401). Upon binding of ligands such as BMP7 or GDF2/BMP9 to the heteromeric complexes, type II receptors transphosphorylate ACVR1 intracellular domain (PubMed:25354296). In turn, ACVR1 kinase domain is activated and subsequently phosphorylates SMAD1/5/8 proteins that transduce the signal (PubMed:9748228). In addition to its role in mediating BMP pathway-specific signaling, suppresses TGFbeta/activin pathway signaling by interfering with the binding of activin to its type II receptor (PubMed:17911401). Besides canonical SMAD signaling, can activate non-canonical pathways such as p38 mitogen-activated protein kinases/MAPKs (By similarity). May promote the expression of HAMP, potentially via its interaction with BMP6 (By similarity).
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Uniprot ID
Q04771
Ensembl ID
ENSG00000115170
HGNC ID
HGNC:171
Subcellular Location
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: CL000025 , HEK-293T
Compound ID Compound Name Compound Formula
CP0143998
1-[4-[6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C25H29N3O3
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0143999
2,6-dimethoxy-4-[4-methyl-5-[4-(4-methylpiperazin-1-yl)phenyl]pyridin-3-yl]benzamide
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C26H30N4O3
 3
1 IC50 < 2 nM
2 IC50 < 3 nM
3 IC50 = 4 nM
CP0250231
2-chloro-6-methoxy-4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C24H25ClN4O2
 4
1 IC50 < 2 nM
2 IC50 = 4 nM
3 IC50 = 5 nM
4 IC50 = 9 nM
CP0574416
8-amino-2-cyclohexyl-5-[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]-3,4-dihydro-2,7-naphthyridin-1-one
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C23H32N6O
 1
1 IC50 = 2.9 nM
CP0125897
2-fluoro-6-methoxy-4-[4-methyl-5-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pyridin-3-yl]benzamide
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C27H31FN4O2
 4
1 IC50 = 3 nM
2 IC50 = 5 nM
3 IC50 = 6 nM
4 IC50 = 83 nM
CP0125898
2-fluoro-6-methoxy-4-[4-methyl-5-[4-(4-methylpiperazin-1-yl)phenyl]pyridin-3-yl]benzamide
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C25H27FN4O2
 4
1 IC50 = 3 nM
2 IC50 = 16 nM
3 IC50 = 17 nM
4 IC50 = 19 nM
CP0143995
2,6-dimethoxy-4-[4-methyl-5-[4-[(3R,5S)-3,4,5-trimethylpiperazin-1-yl]phenyl]pyridin-3-yl]benzamide
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C28H34N4O3
 1
1 IC50 = 3 nM
CP0337570
3-(4-piperazin-1-ylphenyl)-5-(3,4,5-trimethoxyphenyl)pyridine-4-carbonitrile
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C25H26N4O3
 1
1 IC50 = 3 nM
CP0579053
8-amino-2-cyclohexyl-5-(1-piperidin-4-ylpyrazol-4-yl)-3,4-dihydro-2,7-naphthyridin-1-one
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C22H30N6O
 1
1 IC50 = 3.2 nM
CP0579789
8-amino-2-cyclohexyl-5-(1-piperidin-3-ylpyrazol-4-yl)-3,4-dihydro-2,7-naphthyridin-1-one
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C22H30N6O
 1
1 IC50 = 3.5 nM
CP0204819
2-fluoro-6-methoxy-4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C24H25FN4O2
 4
1 IC50 = 4 nM
2 IC50 = 7 nM
3 IC50 = 8 nM
4 IC50 = 24 nM
CP0351989
N,N-dimethyl-4-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine-1-carboxamide
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C28H34N4O4
 1
1 IC50 = 4 nM
CP0579052
8-amino-2-cyclohexyl-5-[1-(piperidin-4-ylmethyl)pyrazol-4-yl]-3,4-dihydro-2,7-naphthyridin-1-one
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C23H32N6O
 1
1 IC50 = 4.4 nM
CP0125900
2-methoxy-4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C24H26N4O2
 3
1 IC50 = 5 nM
2 IC50 = 9 nM
3 IC50 = 17 nM
CP0164881
2,6-dimethoxy-4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C25H28N4O3
 1
1 IC50 = 5 nM
CP0204821
2,6-dimethoxy-4-[4-methyl-5-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]pyridin-3-yl]benzamide
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C28H34N4O3
 1
1 IC50 = 5 nM
CP0367669
4-methyl-3-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-5-(3,4,5-trimethoxyphenyl)pyridine
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C26H28N2O3
 1
1 IC50 = 5 nM
CP0567709
2-(2-adamantyl)-8-amino-5-(1-piperidin-4-ylpyrazol-4-yl)-3,4-dihydro-2,7-naphthyridin-1-one
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C26H34N6O
 1
1 IC50 = 5.3 nM
CP0096946
4-methyl-3-(4-piperidin-4-yloxyphenyl)-5-(3,4,5-trimethoxyphenyl)pyridine
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C26H30N2O4
 1
1 IC50 = 6 nM
CP0564416
4-methyl-3-[4-(1-methylpiperidin-4-yl)oxyphenyl]-5-(3,4,5-trimethoxyphenyl)pyridine
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C27H32N2O4
 1
1 IC50 = 6 nM
CP0579051
8-amino-2-cyclohexyl-5-[1-(piperidin-3-ylmethyl)pyrazol-4-yl]-3,4-dihydro-2,7-naphthyridin-1-one
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C23H32N6O
 1
1 IC50 = 6.5 nM
CP0121895
1-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]-4-propan-2-ylpiperazine
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C28H35N3O3
 1
1 IC50 = 7 nM
CP0232967
4-methyl-3-[4-(1-methylpiperidin-4-yl)phenyl]-5-(3,4,5-trimethoxyphenyl)pyridine
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C27H32N2O3
 1
1 IC50 = 7 nM
CP0111826
1-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C25H29N3O3
 3
1 IC50 = 8 nM
2 IC50 = 9 nM
3 IC50 = 13 nM
CP0163624
(3R,5S)-3,5-dimethyl-1-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C27H33N3O3
 1
1 IC50 = 8 nM
CP0572653
3-amino-6-[2-chloro-4-[(4-morpholin-4-ylpiperidin-1-yl)methyl]phenyl]-N-(4-hydroxy-1-bicyclo[2.2.2]octanyl)pyrazine-2-carboxamide
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C29H39ClN6O3
 2
1 IC50 = 8 nM
2 IC50 = 12 nM
CP0163625
4-methyl-3-(4-piperidin-4-ylphenyl)-5-(3,4,5-trimethoxyphenyl)pyridine
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C26H30N2O3
 1
1 IC50 = 9 nM
CP0561826
1-methyl-4-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C26H31N3O3
 1
1 IC50 = 9 nM
CP0125896
2-fluoro-6-methoxy-4-[4-methyl-5-[4-[(3R,5S)-3,4,5-trimethylpiperazin-1-yl]phenyl]pyridin-3-yl]benzamide
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C27H31FN4O2
 1
1 IC50 = 10 nM
CP0572899
3-amino-N-cyclohexyl-6-[4-[(dimethylamino)methyl]phenyl]pyrazine-2-carboxamide
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C20H27N5O
 1
1 IC50 = 10 nM
CP0258427
3-(4-fluoro-3,5-dimethoxyphenyl)-5-(4-piperazin-1-ylphenyl)pyridine-4-carbonitrile
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C24H23FN4O2
 1
1 IC50 = 11 nM
CP0579443
CHEMBL5189710
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C25H36N6O2
 1
1 IC50 = 11 nM
CP0579477
8-amino-2-cyclobutyl-5-(1-piperidin-4-ylpyrazol-4-yl)-3,4-dihydro-2,7-naphthyridin-1-one
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C20H26N6O
 1
1 IC50 = 11 nM
CP0330124
1-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]-1,4-diazepane
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C26H31N3O3
 1
1 IC50 = 13 nM
CP0525937
4-methyl-3-[4-(1-methyl-3,6-dihydro-2H-pyridin-4-yl)phenyl]-5-(3,4,5-trimethoxyphenyl)pyridine
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C27H30N2O3
 1
1 IC50 = 14 nM
CP0128561
1-[4-[5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C24H27N3O3
 2
1 IC50 = 15 nM
2 IC50 = 18 nM
CP0329734
1-[4-[4-fluoro-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C24H26FN3O3
 1
1 IC50 = 15 nM
CP0232965
1-[4-[4-chloro-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C24H26ClN3O3
 1
1 IC50 = 16 nM
CP0330123
4-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]-1,4-thiazinane 1,1-dioxide
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C25H28N2O5S
 1
1 IC50 = 16 nM
CP0258428
1-(2-fluoroethyl)-4-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C27H32FN3O3
 1
1 IC50 = 17 nM
CP0572569
CHEMBL5206645
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C27H40N6O2
 1
1 IC50 = 17 nM
CP0579475
5-[1-(1-acetylpiperidin-4-yl)pyrazol-4-yl]-8-amino-2-cyclohexyl-3,4-dihydro-2,7-naphthyridin-1-one
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C24H32N6O2
 1
1 IC50 = 17 nM
CP0232970
1-[4-[5-(4-fluoro-3,5-dimethoxyphenyl)-4-methylpyridin-3-yl]phenyl]piperazine
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C24H26FN3O2
 1
1 IC50 = 19 nM
CP0572570
CHEMBL5199857
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C27H38N6O3
 1
1 IC50 = 19 nM
CP0573938
CHEMBL5204737
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C27H37ClN6O3
 1
1 IC50 = 19 nM
CP0163626
1-methyl-4-[[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]methyl]piperazine
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C27H33N3O3
 1
1 IC50 = 20 nM
CP0567708
8-amino-2-cyclohexyl-5-[1-(oxetan-3-yl)pyrazol-4-yl]-3,4-dihydro-2,7-naphthyridin-1-one
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C20H25N5O2
 1
1 IC50 = 21 nM
CP0574417
8-amino-2-(4-hydroxy-4-methylcyclohexyl)-5-(1-piperidin-4-ylpyrazol-4-yl)-3,4-dihydro-2,7-naphthyridin-1-one
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C23H32N6O2
 1
1 IC50 = 21 nM
CP0423902
1-[4-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazin-1-yl]ethanone
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C27H31N3O4
 1
1 IC50 = 22 nM
CP0580164
3-amino-6-[4-[(dimethylamino)methyl]phenyl]-N-(4-hydroxycyclohexyl)pyrazine-2-carboxamide
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C20H27N5O2
 1
1 IC50 = 22 nM
CP0567707
8-amino-2-cyclohexyl-5-(1-cyclopentylpyrazol-4-yl)-3,4-dihydro-2,7-naphthyridin-1-one
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C22H29N5O
 1
1 IC50 = 22 nM
CP0143998
1-[4-[6-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C25H29N3O3
 2
1 IC50 = 24 nM
2 IC50 = 115 nM
CP0579342
8-amino-2-cyclohexyl-5-(1-propan-2-ylpyrazol-4-yl)-3,4-dihydro-2,7-naphthyridin-1-one
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C20H27N5O
 1
1 IC50 = 25 nM
CP0409304
4-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]morpholine
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C25H28N2O4
 1
1 IC50 = 28 nM
CP0516506
1-methylsulfonyl-4-[4-[4-methyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C26H31N3O5S
 1
1 IC50 = 29 nM
CP0577106
3-amino-6-[4-[(4-propan-2-ylpiperazin-1-yl)methyl]phenyl]-N-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]pyrazine-2-carboxamide
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C23H31F3N6O2
 1
1 IC50 = 33 nM
CP0351988
1-[4-[5-(3,5-dimethoxyphenyl)-4-methylpyridin-3-yl]phenyl]piperazine
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C24H27N3O2
 1
1 IC50 = 39 nM
CP0258425
1-[4-[4-cyclopropyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C27H31N3O3
 1
1 IC50 = 42 nM
CP0578701
3-amino-6-[4-[(dimethylamino)methyl]phenyl]-N-(2-hydroxycyclopentyl)pyrazine-2-carboxamide
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C19H25N5O2
 1
1 IC50 = 48 nM
CP0571733
3-amino-6-[4-[(dimethylamino)methyl]phenyl]-N-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]pyrazine-2-carboxamide
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C18H22F3N5O2
 1
1 IC50 = 49 nM
CP0571120
3-amino-6-[4-(piperazin-1-ylmethyl)phenyl]-N-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]pyrazine-2-carboxamide
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C20H25F3N6O2
 1
1 IC50 = 50 nM
CP0578380
CHEMBL5196823
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C28H39ClN6O3
 1
1 IC50 = 50 nM
CP0520843
1-[4-[4-(trifluoromethyl)-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C25H26F3N3O3
 1
1 IC50 = 67 nM
CP0579343
8-amino-5-(1-piperidin-4-ylpyrazol-4-yl)-2-propan-2-yl-3,4-dihydro-2,7-naphthyridin-1-one
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C19H26N6O
 1
1 IC50 = 72 nM
CP0579947
3-amino-6-[4-[(dimethylamino)methyl]phenyl]-N-propan-2-ylpyrazine-2-carboxamide
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C17H23N5O
 1
1 IC50 = 73 nM
CP0569242
3-amino-6-[4-[(1,1-dioxo-1,4-thiazinan-4-yl)methyl]phenyl]-N-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]pyrazine-2-carboxamide
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C20H24F3N5O4S
 1
1 IC50 = 76 nM
CP0545294
3-amino-6-[4-(morpholin-4-ylmethyl)phenyl]-N-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]pyrazine-2-carboxamide
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C20H24F3N5O3
 1
1 IC50 = 90 nM
CP0571119
3-amino-6-[4-[(dimethylamino)methyl]phenyl]-N-ethylpyrazine-2-carboxamide
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C16H21N5O
 1
1 IC50 = 100 nM
CP0577105
3-amino-6-[4-(diethylaminomethyl)phenyl]-N-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]pyrazine-2-carboxamide
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C20H26F3N5O2
 1
1 IC50 = 100 nM
CP0577743
3-amino-6-[4-(pyrrolidin-1-ylmethyl)phenyl]-N-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropyl]pyrazine-2-carboxamide
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C20H24F3N5O2
 1
1 IC50 = 100 nM
CP0263439
3-methoxy-5-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C24H26N4O2
 1
1 IC50 = 102 nM
CP0567778
1-[4-[4-methoxy-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C25H29N3O4
 1
1 IC50 = 103 nM
CP0580163
3-amino-6-[4-[(dimethylamino)methyl]phenyl]-N-(2-hydroxypropyl)pyrazine-2-carboxamide
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C17H23N5O2
 1
1 IC50 = 110 nM
CP0577904
3-amino-6-[4-[(dimethylamino)methyl]phenyl]-N-(3,3,3-trifluoro-2-hydroxypropyl)pyrazine-2-carboxamide
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C17H20F3N5O2
 1
1 IC50 = 140 nM
CP0158027
5-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]-2,3-dihydroisoindol-1-one
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C24H24N4O
 4
1 IC50 = 171 nM
2 IC50 = 226 nM
3 IC50 = 363 nM
4 IC50 = 652 nM
CP0330120
1-[4-[4-ethyl-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenyl]piperazine
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C26H31N3O3
 1
1 IC50 = 181 nM
CP0204820
2-fluoro-4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C23H23FN4O
 1
1 IC50 = 263 nM
CP0561825
3-(4-piperazin-1-ylphenyl)-5-(3,4,5-trimethoxyphenyl)pyridin-4-amine
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C24H28N4O3
 1
1 IC50 = 461 nM
CP0143993
4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C23H24N4O
 1
1 IC50 = 477 nM
CP0143996
2-(methoxymethyl)-4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C25H28N4O2
 1
1 IC50 = 687 nM
CP0143994
3-methoxy-4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]thiophene-2-carboxamide
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C22H24N4O2S
 1
1 IC50 = 712 nM
CP0223091
3-methoxy-5-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]thiophene-2-carboxamide
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C22H24N4O2S
 1
1 IC50 = 751 nM
CP0064594
4-methoxy-5-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]thiophene-3-carboxamide
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C22H24N4O2S
 1
1 IC50 > 1000 nM
CP0143997
2-methoxy-5-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C24H26N4O2
 1
1 IC50 > 1000 nM
CP0164880
2-methoxy-N-methyl-4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C25H28N4O2
 1
1 IC50 > 1000 nM
CP0249538
2-methoxy-N,N-dimethyl-4-[4-methyl-5-(4-piperazin-1-ylphenyl)pyridin-3-yl]benzamide
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C26H30N4O2
 1
1 IC50 > 1000 nM
Clinical Information about the Protein
Target 1 ( Activin receptor-like kinase 2 (ALK-2) )
Target Type Clinical trial Target