Reaction Details Report a problem with these data
Target
Activin receptor type-1 [R206H]
Ligand
BDBM488054
Substrate
n/a
Meas. Tech.
Enzyme Inhibitory Assay
IC50
6.70±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:
BDBM488054
Synonyms:
2-Methyl-1-(4-(2-((2- methyl-1,2,3,4- tetrahydroisoquinolin- 6-yl)amino)pyrimidin- 4-yl)-3-(pyridin-3-yl)- 1H-pyrazol-1- yl)propan-2-ol | US10954216, Example 65
Type:
Small organic molecule
Emp. Form.:
C26H29N7O
Mol. Mass.:
455.5548
SMILES:
CN1CCc2cc(Nc3nccc(n3)-c3cn(CC(C)(C)O)nc3-c3cccnc3)ccc2C1
Structure:
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