Ki Summary

Reaction Details

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Target

Proteinase-activated receptor 1

Ligand

BDBM50261018

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_556010 (CHEMBL964660)

6.5±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

BDBM50261018

n/a

Name

BDBM50261018

Synonyms:

CHEMBL494618 | N-((1R,3aR,4aR,6R,8aR,9S,9aS)-9-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-1-methyl-3-oxo-dodecahydronaphtho[2,3-c]furan-6-yl)cyclopropanecarboxamide

Type

Small organic molecule

Emp. Form.

C30H33FN2O3

Mol. Mass.

488.593

SMILES

C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@@H](CC[C@H]3[C@H](\C=C\c3ccc(cn3)-c3cccc(F)c3)[C@H]12)NC(=O)C1CC1 |r|

Structure