Ki Summary

Reaction Details

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Target

Proteinase-activated receptor 1

Ligand

BDBM50585042

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_2161343 (CHEMBL5046093)

IC50

4.0±n/a nM

Citation

Mandal, M; Madeira, M; Amin, RP; Buevich, AV; Cheng, A; Labroli, M; Liu, X; Acton, J; Pio, B; Basso, A; Chobanian, H; Dong, G; Dropinski, J; Guo, Y; Guo, Z; Kurowski, S; Korfmacher, W; Lee, S; Meng, D; Ondeyka, D; Yang, Z; Zhang, R; Wei, H; Wu, Z; Zhang, F; Wollenberg, G; Biftu, T; Greenlee, WJ; Chintala, M; Maletic, M; Zhu, Z Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery. J Med Chem65:5575-5592 (2022) [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

BDBM50585042

n/a

Name

BDBM50585042

Synonyms:

CHEMBL5069528

Type

Small organic molecule

Emp. Form.

C30H33N3O4

Mol. Mass.

499.6007

SMILES

[H][C@@]12[C@@H](C)OC(=O)[C@@]11CN(C[C@H]1[C@H](C)[C@@H](C)[C@@H]2\C=C\c1ccc(cn1)-c1ccccc1C#N)C(=O)OCC |r|

Structure