Reaction Details Report a problem with these data
Target
Activin receptor type-1 [R206H]
Ligand
BDBM488044
Substrate
n/a
Meas. Tech.
Enzyme Inhibitory Assay
IC50
24.9±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:
BDBM488044
Synonyms:
4-(1-Ethyl-3-(pyridin- 3-yl)-1H-pyrazol-4- yl)-N-(4-(2-(4-(2- methoxyethyl)piperazin-1- yl)ethyl)phenyl)pyrimidin- 2-amine | US10954216, Example 43
Type:
Small organic molecule
Emp. Form.:
C29H36N8O
Mol. Mass.:
512.6491
SMILES:
CCn1cc(c(n1)-c1cccnc1)-c1ccnc(Nc2ccc(CCN3CCN(CCOC)CC3)cc2)n1
Structure:
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