Reaction Details Report a problem with these data
Target
Activin receptor type-1 [R206H]
Ligand
BDBM488039
Substrate
n/a
Meas. Tech.
Enzyme Inhibitory Assay
IC50
5.70±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:
BDBM488039
Synonyms:
N-(4-(4- (Cyclopropylmethyl) piperazin-1-yl)phenyl)- 4-(1-ethyl-3-(pyridin- 3-yl)-1H-pyrazol-4- yl)pyrimidin-2-amine | US10954216, Example 33
Type:
Small organic molecule
Emp. Form.:
C28H32N8
Mol. Mass.:
480.6073
SMILES:
CCn1cc(c(n1)-c1cccnc1)-c1ccnc(Nc2ccc(cc2)N2CCN(CC3CC3)CC2)n1
Structure:
Search PDB for entries with ligand similarity: