Reaction Details Report a problem with these data
Target
Platelet-activating factor receptor
Ligand
BDBM50000714
Substrate
n/a
Meas. Tech.
ChEMBL_158343 (CHEMBL768487)
IC50
94±n/a nM
Citation
Cai, X; Scannell, RT; Yaeger, D; Hussoin, MS; Killian, DB; Qian, C; Eckman, J; Hwang, SB; Libertine-Garahan, L; Yeh, CG; Ip, SH; Shen, TY (+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist. J Med Chem 41:1970-9 (1998) [PubMed] Article
More Info.:
Target
Name:
Platelet-activating factor receptor
Synonyms:
PAF Platelet activating factor | PAF-R | PAFR | PTAFR | PTAFR_HUMAN | Platelet activating factor receptor | Platelet-activating factor receptor
Type:
Enzyme Catalytic Domain
Mol. Mass.:
39219.60
Organism:
Human
Description:
PAF Platelet activating factor PTAFR HUMAN::P25105
Residue:
342
Sequence:
MEPHDSSHMDSEFRYTLFPIVYSIIFVLGVIANGYVLWVFARLYPCKKFNEIKIFMVNLTMADMLFLITLPLWIVYYQNQGNWILPKFLCNVAGCLFFINTYCSVAFLGVITYNRFQAVTRPIKTAQANTRKRGISLSLVIWVAIVGAASYFLILDSTNTVPDSAGSGNVTRCFEHYEKGSVPVLIIHIFIVFSFFLVFLIILFCNLVIIRTLLMQPVQQQRNAEVKRRALWMVCTVLAVFIICFVPHHVVQLPWTLAELGFQDSKFHQAINDAHQVTLCLLSTNCVLDPVIYCFLTKKFRKHLTEKFYSMRSSRKCSRATTDTVTEVVVPFNQIPGNSLKN
Inhibitor
Name:
BDBM50000714
Synonyms:
3-[4-(2-Chloro-phenyl)-9-methyl-6H-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulen-2-yl]-1-morpholin-4-yl-propan-1-one | 3-[4-(2-Chloro-phenyl)-9-methyl-6H-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulen-2-yl]-1-morpholin-4-yl-propan-1-one(WEB 2086) | 3-[4-(2-Chloro-phenyl)-9-methyl-6H-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulen-2-yl]-1-morpholin-4-yl-propan-1-one(WEB2086) | Apafant | CHEMBL280164 | WEB2086
Type:
Small organic molecule
Emp. Form.:
C22H22ClN5O2S
Mol. Mass.:
455.96
SMILES:
Cc1nnc2CN=C(c3cc(CCC(=O)N4CCOCC4)sc3-n12)c1ccccc1Cl |c:6|