Reaction Details Report a problem with these data
Target
Activin receptor type-1 [R206H]
Ligand
BDBM488030
Substrate
n/a
Meas. Tech.
Enzyme Inhibitory Assay
IC50
18.7±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:
BDBM488030
Synonyms:
2-Methyl-N-(4-(1- (oxetan-3-yl)-3- (pyridin-3-yl)-1H- pyrazol-4- yl)pyrimidin-2-yl)- 1,2,3,4- tetrahydroisoquinolin- 6-amine | US10954216, Example 8
Type:
Small organic molecule
Emp. Form.:
C25H25N7O
Mol. Mass.:
439.5123
SMILES:
CN1CCc2cc(Nc3nccc(n3)-c3cn(nc3-c3cccnc3)C3COC3)ccc2C1
Structure:
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