Ki Summary

Reaction Details

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Target

Proteinase-activated receptor 1

Ligand

BDBM50261116

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_556010 (CHEMBL964660)

3.7±n/a nM

Citation

Chackalamannil, S; Wang, Y; Greenlee, WJ; Hu, Z; Xia, Y; Ahn, HS; Boykow, G; Hsieh, Y; Palamanda, J; Agans-Fantuzzi, J; Kurowski, S; Graziano, M; Chintala, M Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem51:3061-4 (2008) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Proteinase-activated receptor 1

Name:

Proteinase-activated receptor 1

Synonyms:

CF2R | Coagulation factor II receptor | F2R | PAR-1 | PAR1 | PAR1_HUMAN | Proteinase activated receptor 1 | Proteinase-activated receptor 1 (PAR-1) | TR | Thrombin receptor | Thrombin receptor/ Proteinase-activated receptor 1(Par-1)

Type:

Protein

Mol. Mass.:

47450.07

Organism:

Homo sapiens (Human)

Description:

P25116

Residue:

425

Sequence:

MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEE
KNESGLTEYRLVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLN
IMAIVVFILKMKVKKPAVVYMLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTA
AFYCNMYASILLMTVISIDRFLAVVYPMQSLSWRTLGRASFTCLAIWALAIAGVVPLLLK
EQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFFVPLIISTVCYVSIIRCLSSS
AVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAYFAYLLCVCVS
SISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIY
KKLLT

BDBM50261116

n/a

Name

BDBM50261116

Synonyms:

CHEMBL453277 | ethyl methyl((1R,3aR,4aR,6R,8aR,9S,9aS)-1-methyl-3-oxo-9-((E)-2-(5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)vinyl)-dodecahydronaphtho[2,3-c]furan-6-yl)carbamate

Type

Small organic molecule

Emp. Form.

C31H35F3N2O4

Mol. Mass.

556.6158

SMILES

CCOC(=O)N(C)[C@@H]1CC[C@@H]2[C@H](C[C@@H]3[C@@H]([C@@H](C)OC3=O)[C@H]2\C=C\c2ccc(cn2)-c2cccc(c2)C(F)(F)F)C1 |r|

Structure