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Assay Detail

CHEMBL676105

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Ability to inhibit binding of [125I]ET1 to membranes prepared from A10 rat thoracic aorta smooth muscle Endothelin A receptor
ChEMBL ↗
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Thoracic aorta
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Endothelin-1 receptor (CHEMBL4566) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).
Murugesan N, Gu Z, Stein PD, Bisaha S, Spergel S, Girotra R, Lee VG, Lloyd J, Misra RN, Schmidt J, Mathur A, Stratton L, Kelly YF, Bird E, Waldron T, Liu EC, Zhang R, Lee H, Serafino R, Abboa-Offei B, Mathers P, Giancarli M, Seymour AA, Webb ML, Hunt JT.
J Med Chem (1998) 41 : 5198 -5218
PubMed 9857090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 75 6.93 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL151440 — — 1 8.70
CHEMBL149819 — — 1 8.57
CHEMBL106684 — — 1 8.33
CHEMBL421955 — — 1 8.30
CHEMBL358254 — — 1 8.30
CHEMBL150474 — — 1 8.20
CHEMBL345542 — — 1 8.19
CHEMBL422851 — — 1 8.10
CHEMBL434082 — — 1 7.89
CHEMBL147081 — — 1 7.85
CHEMBL359167 — — 1 7.85
CHEMBL347958 — — 1 7.80
CHEMBL422128 — — 1 7.80
CHEMBL347982 — — 1 7.77
CHEMBL346853 — — 1 7.77
CHEMBL105490 — — 1 7.75
CHEMBL151160 — — 1 7.70
CHEMBL357395 — — 1 7.70
CHEMBL149953 — — 1 7.55
CHEMBL146845 — — 1 7.54
CHEMBL347125 — — 1 7.50
CHEMBL422496 — — 1 7.48
CHEMBL151422 — — 1 7.47
CHEMBL151926 — — 1 7.43
CHEMBL348685 — — 1 7.41
CHEMBL150891 — — 1 7.40
CHEMBL314691 BQ-123 2.0 1 7.40
CHEMBL149152 — — 1 7.38
CHEMBL149818 — — 1 7.37
CHEMBL348700 — — 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL151440 — Ki = 2.0 nM 8.70
CHEMBL149819 — Ki = 2.7 nM 8.57
CHEMBL106684 — Ki = 4.7 nM 8.33
CHEMBL421955 — Ki = 5.0 nM 8.30
CHEMBL358254 — Ki = 5.0 nM 8.30
CHEMBL150474 — Ki = 6.3 nM 8.20
CHEMBL345542 — Ki = 6.4 nM 8.19
CHEMBL422851 — Ki = 8.0 nM 8.10
CHEMBL434082 — Ki = 13.0 nM 7.89
CHEMBL147081 — Ki = 14.0 nM 7.85
CHEMBL359167 — Ki = 14.0 nM 7.85
CHEMBL347958 — Ki = 16.0 nM 7.80
CHEMBL422128 — Ki = 16.0 nM 7.80
CHEMBL346853 — Ki = 17.0 nM 7.77
CHEMBL347982 — Ki = 17.0 nM 7.77
CHEMBL105490 — Ki = 18.0 nM 7.75
CHEMBL151160 — Ki = 20.0 nM 7.70
CHEMBL357395 — Ki = 20.0 nM 7.70
CHEMBL149953 — Ki = 28.0 nM 7.55
CHEMBL146845 — Ki = 29.0 nM 7.54
CHEMBL347125 — Ki = 32.0 nM 7.50
CHEMBL422496 — Ki = 33.0 nM 7.48
CHEMBL151422 — Ki = 34.0 nM 7.47
CHEMBL151926 — Ki = 37.0 nM 7.43
CHEMBL348685 — Ki = 39.0 nM 7.41
CHEMBL150891 — Ki = 40.0 nM 7.40
CHEMBL314691 BQ-123 Ki = 40.0 nM 7.40
CHEMBL149152 — Ki = 42.0 nM 7.38
CHEMBL149818 — Ki = 43.0 nM 7.37
CHEMBL348700 — Ki = 50.0 nM 7.30
CHEMBL343867 — Ki = 50.0 nM 7.30
CHEMBL356901 — Ki = 54.0 nM 7.27
CHEMBL267458 BMS-182874 Ki = 55.0 nM 7.26
CHEMBL358020 — Ki = 55.0 nM 7.26
CHEMBL149241 — Ki = 60.0 nM 7.22
CHEMBL151971 — Ki = 61.0 nM 7.21
CHEMBL424504 — Ki = 62.0 nM 7.21
CHEMBL148853 — Ki = 74.0 nM 7.13
CHEMBL345551 — Ki = 80.0 nM 7.10
CHEMBL310427 — Ki = 90.0 nM 7.05
CHEMBL357823 — Ki = 89.0 nM 7.05
CHEMBL146904 — Ki = 100.0 nM 7.00
CHEMBL423583 — Ki = 100.0 nM 7.00
CHEMBL359332 — Ki = 103.0 nM 6.99
CHEMBL149050 — Ki = 110.0 nM 6.96
CHEMBL358545 — Ki = 110.0 nM 6.96
CHEMBL356591 — Ki = 112.0 nM 6.95
CHEMBL357580 — Ki = 140.0 nM 6.85
CHEMBL147521 — Ki = 190.0 nM 6.72
CHEMBL358226 — Ki = 190.0 nM 6.72