Reaction Details Report a problem with these data
Target
Activin receptor type-1 [R206H]
Ligand
BDBM488058
Substrate
n/a
Meas. Tech.
Enzyme Inhibitory Assay
IC50
1.30±n/a nM
Citation
 Hashizume, Y; Sekimata, K; Kubota, H; Yamamoto, H; Koda, Y; Koyama, H; Taguri, T; Sato, T; Tanaka, A; Miyazono, K BMP-signal-inhibiting compound US Patent  US10954216 Publication Date 3/23/2021 
Target
Name:
Activin receptor type-1 [R206H]
Synonyms:
ACVR1 | ACVR1_HUMAN | ACVRLK2 | Activin receptor type-1 (ALK-2)(R206H)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
57138.77
Organism:
Homo sapiens (Human)
Description:
Q04771[R206H]
Residue:
509
Sequence:
MVDGVMILPVLIMIALPSPSMEDEKPKVNPKLYMCVCEGLSCGNEDHCEGQQCFSSLSINDGFHVYQKGCFQVYEQGKMTCKTPPSPGQAVECCQGDWCNRNITAQLPTKGKSFPGTQNFHLEVGLIILSVVFAVCLLACLLGVALRKFKRRNQERLNPRDVEYGTIEGLITTNVGDSTLADLLDHSCTSGSGSGLPFLVQRTVAHQITLLECVGKGRYGEVWRGSWQGENVAVKIFSSRDEKSWFRETELYNTVMLRHENILGFIASDMTSRHSSTQLWLITHYHEMGSLYDYLQLTTLDTVSCLRIVLSIASGLAHLHIEIFGTQGKPAIAHRDLKSKNILVKKNGQCCIADLGLAVMHSQSTNQLDVGNNPRVGTKRYMAPEVLDETIQVDCFDSYKRVDIWAFGLVLWEVARRMVSNGIVEDYKPPFYDVVPNDPSFEDMRKVVCVDQQRPNIPNRWFSDPTLTSLAKLMKECWYQNPSARLTALRIKKTLTKIDNSLDKLKTDC
  
Inhibitor
Name:
BDBM488058
Synonyms:
N-(4-(4-(2- Methoxyethyl)piperazin- 1-yl)phenyl)-4-(3- (pyridin-3-yl)-1- (tetrahydrofuran-3- yl)-1H-pyrazol-4- yl)pyrimidin-2-amine | US10954216, Example 76
Type:
Small organic molecule
Emp. Form.:
C29H34N8O2
Mol. Mass.:
526.6327
SMILES:
COCCN1CCN(CC1)c1ccc(Nc2nccc(n2)-c2cn(nc2-c2cccnc2)C2CCOC2)cc1
Structure:
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