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Assay Detail

CHEMBL649312

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

Binding
Binding affinity for Angiotensin II receptor, type 1 in rat adrenal cortical membranes using [125I]Sar1, Ile8-angiotensin II
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Quinoxaline N-oxide containing potent angiotensin II receptor antagonists: synthesis, biological properties, and structure-activity relationships.
Kim KS, Qian L, Bird JE, Dickinson KE, Moreland S, Schaeffer TR, Waldron TL, Delaney CL, Weller HN, Miller AV.
J Med Chem (1993) 36 : 2335 -2342
PubMed 8360878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.42 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312066 1 8.89
CHEMBL77029 1 8.35
CHEMBL77935 1 8.13
CHEMBL77827 1 8.05
CHEMBL306278 1 7.82
CHEMBL75053 1 7.77
CHEMBL74445 1 7.68
CHEMBL312068 1 7.66
CHEMBL77376 1 7.55
CHEMBL309489 1 7.36
CHEMBL76785 1 7.34
CHEMBL76765 1 7.30
CHEMBL433310 1 7.17
CHEMBL75101 1 7.15
CHEMBL76943 1 6.86
CHEMBL77266 1 6.72
CHEMBL77185 1 6.26
CHEMBL307946 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312066 Ki = 1.3 nM 8.89
CHEMBL77029 Ki = 4.5 nM 8.35
CHEMBL77935 Ki = 7.4 nM 8.13
CHEMBL77827 Ki = 9.0 nM 8.05
CHEMBL306278 Ki = 15.0 nM 7.82
CHEMBL75053 Ki = 17.0 nM 7.77
CHEMBL74445 Ki = 21.0 nM 7.68
CHEMBL312068 Ki = 22.0 nM 7.66
CHEMBL77376 Ki = 28.0 nM 7.55
CHEMBL309489 Ki = 44.0 nM 7.36
CHEMBL76785 Ki = 46.0 nM 7.34
CHEMBL76765 Ki = 50.0 nM 7.30
CHEMBL433310 Ki = 68.0 nM 7.17
CHEMBL75101 Ki = 71.0 nM 7.15
CHEMBL76943 Ki = 137.0 nM 6.86
CHEMBL77266 Ki = 190.0 nM 6.72
CHEMBL77185 Ki = 550.0 nM 6.26
CHEMBL307946 Ki = 3450.0 nM 5.46