Ki Summary

Reaction Details

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Target

Endothelin-1 receptor

Ligand

BDBM50091105

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_63370 (CHEMBL676106)

1.4±n/a nM

Citation

Wu, C; Decker, ER; Blok, N; Bui, H; You, TJ; Wang, J; Bourgoyne, AR; Knowles, V; Berens, KL; Holland, GW; Brock, TA; Dixon, RA Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. J Med Chem47:1969-86 (2004) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Endothelin-1 receptor

Name:

Endothelin-1 receptor

Synonyms:

EDNRA_RAT | ENDOTHELIN A | Ednra | Endothelin receptor | Endothelin-1 receptor

Type:

Enzyme Catalytic Domain

Mol. Mass.:

48256.91

Organism:

RAT

Description:

ENDOTHELIN A EDNRA RAT::P26684

Residue:

426

Sequence:

MGVLCFLASFWLALVGGAIADNAERYSANLSSHVEDFTPFPGTEFNFLGTTLQPPNLALP
SNGSMHGYCPQQTKITTAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIA
SLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALS
VDRYRAVASWSRVQGIGIPLITAIEIVSIWILSFILAIPEAIGFVMVPFEYKGEQHRTCM
LNATTKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQ
RREVAKTVFCLVVIFALCWFPLHLSRILKKTVYDEMDKNRCELLSFLLLMDYIGINLATM
NSCINPIALYFVSKKFKNCFQSCLCCCCHQSKSLMTSVPMNGTSIQWKNQEQNHNTERSS
HKDSMN

BDBM50091105

n/a

Name

BDBM50091105

Synonyms:

4''-Oxazol-2-yl-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide | 4'-Oxazol-2-yl-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide | 4'-Oxazol-2-yl-biphenyl-2-sulfonicacid(3,4-dimethyl-isoxazol-5-yl)-amide | BMS-193884 | CHEMBL24461

Type

Small organic molecule

Emp. Form.

C20H17N3O4S

Mol. Mass.

395.432

SMILES

Cc1noc(NS(=O)(=O)c2ccccc2-c2ccc(cc2)-c2ncco2)c1C

Structure