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Assay Detail

CHEMBL648767

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

Binding
Binding affinity for Angiotensin II receptor, type 1 determined using [125I]- labeled [Sar1,Ile8] angiotensin II in rat adrenocortical membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Type-1 angiotensin II receptor B (CHEMBL263)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1,4-substituted indoles: a potent and selective class of angiostensin II receptor antagonists
Poss MA, Gu Z, Ryono DE, Reid JA, Sieber-McMaster E, Spitzmiller ER, Dejneka T, Dickinson KE, Williams SB, Moreland S, Delaney CL, Bird J, Waldron TL, Schaeffer TR, Hedberg S, Petrillo EW
Bioorg Med Chem Lett (1994) 4 : 145 -150
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.34 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4524047 1 9.10
CHEMBL2079784 1 8.35
CHEMBL2021415 1 8.20
CHEMBL1790055 1 8.20
CHEMBL2079782 1 8.14
CHEMBL2079781 1 8.05
CHEMBL2079769 1 7.89
CHEMBL2021416 1 7.60
CHEMBL2079768 1 7.52
CHEMBL2079770 1 7.41
CHEMBL288691 1 7.10
CHEMBL4524049 1 7.10
CHEMBL287065 1 6.12
CHEMBL4524048 1 6.08
CHEMBL433230 1 5.44
CHEMBL36259 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4524047 Ki = 0.8 nM 9.10
CHEMBL2079784 Ki = 4.5 nM 8.35
CHEMBL2021415 Ki = 6.3 nM 8.20
CHEMBL1790055 Ki = 6.3 nM 8.20
CHEMBL2079782 Ki = 7.3 nM 8.14
CHEMBL2079781 Ki = 8.9 nM 8.05
CHEMBL2079769 Ki = 13.0 nM 7.89
CHEMBL2021416 Ki = 25.0 nM 7.60
CHEMBL2079768 Ki = 30.0 nM 7.52
CHEMBL2079770 Ki = 39.0 nM 7.41
CHEMBL288691 Ki = 79.0 nM 7.10
CHEMBL4524049 Ki = 79.0 nM 7.10
CHEMBL287065 Ki = 760.0 nM 6.12
CHEMBL4524048 Ki = 840.0 nM 6.08
CHEMBL433230 Ki = 3600.0 nM 5.44
CHEMBL36259 Ki = 6100.0 nM 5.21