Ki Summary

Reaction Details

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Target

Proteinase-activated receptor 1

Ligand

BDBM50202067

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_423382 (CHEMBL909901)

IC50

16.5±n/a nM

Citation

Clasby, MC; Chackalamannil, S; Czarniecki, M; Doller, D; Eagen, K; Greenlee, W; Kao, G; Lin, Y; Tsai, H; Xia, Y; Ahn, HS; Agans-Fantuzzi, J; Boykow, G; Chintala, M; Foster, C; Smith-Torhan, A; Alton, K; Bryant, M; Hsieh, Y; Lau, J; Palamanda, J Metabolism-based identification of a potent thrombin receptor antagonist. J Med Chem50:129-38 (2007) [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

BDBM50202067

n/a

Name

BDBM50202067

Synonyms:

(3R,3aS,4S,4aR,7R,8aR,9aR)-decahydro-7-hydroxy-3-methyl-4-[(E)-2-[5-(2,3-dichlorophenyl)-2-pyridinyl]ethenyl]naphtho-[2,3-c]furan-1(3H)-one | CHEMBL374503

Type

Small organic molecule

Emp. Form.

C26H27Cl2NO3

Mol. Mass.

472.403

SMILES

C[C@H]1OC(=O)[C@@H]2C[C@@H]3C[C@H](O)CC[C@H]3[C@H](\C=C\c3ccc(cn3)-c3cccc(Cl)c3Cl)[C@H]12 |r|

Structure