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Assay Detail

CHEMBL1043589

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

Binding
Displacement of [125I]SI-Ang2 from AT1 receptor in Sprague-Dawley rat liver membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Type-1 angiotensin II receptor A (CHEMBL329)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and docking studies of novel benzimidazoles for the treatment of metabolic syndrome.
Mizuno CS, Chittiboyina AG, Shah FH, Patny A, Kurtz TW, Pershadsingh HA, Speth RC, Karamyan VT, Carvalho PB, Avery MA.
J Med Chem (2010) 53 : 1076 -1085
PubMed 20073471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.49 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1017 TELMISARTAN 4.0 1 9.64
CHEMBL566614 1 7.87
CHEMBL567898 1 5.79
CHEMBL572276 1 5.65
CHEMBL571763 1 5.60
CHEMBL567897 1 5.55
CHEMBL567054 1 5.30
CHEMBL567063 1 -
CHEMBL567689 1 -
CHEMBL565793 1 -
CHEMBL565379 1 -
CHEMBL567269 1 -
CHEMBL584704 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1017 TELMISARTAN Ki = 0.23 nM 9.64
CHEMBL566614 Ki = 13.4 nM 7.87
CHEMBL567898 Ki = 1618.0 nM 5.79
CHEMBL572276 Ki = 2226.0 nM 5.65
CHEMBL571763 Ki = 2534.0 nM 5.60
CHEMBL567897 Ki = 2840.0 nM 5.55
CHEMBL567054 Ki = 5060.0 nM 5.30
CHEMBL567063 Ki > 10000.0 nM -
CHEMBL567689 Ki > 10000.0 nM -
CHEMBL565793 Ki > 10000.0 nM -
CHEMBL565379 Ki > 10000.0 nM -
CHEMBL567269 Ki > 10000.0 nM -
CHEMBL584704 Ki > 10000.0 nM -