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Assay Detail

CHEMBL649313

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

Binding
Binding affinity towards Angiotensin II receptor, type 1 in rat aortic smooth muscle cells using 0.2 nM [125I]-labeled Sar-Ile-angiotensin II
25
Total Activities
25
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

Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.
Tellew JE, Baska RA, Beyer SM, Carlson KE, Cornelius LA, Fadnis L, Gu Z, Kunst BL, Kowala MC, Monshizadegan H, Murugesan N, Ryan CS, Valentine MT, Yang Y, Macor JE.
Bioorg Med Chem Lett (2003) 13 : 1093 -1096
PubMed 12643919 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.03 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11840 1 9.22
CHEMBL12233 1 8.89
CHEMBL12588 1 8.70
CHEMBL12013 1 8.70
CHEMBL12106 1 8.70
CHEMBL12175 1 8.52
CHEMBL266628 1 8.40
CHEMBL268706 1 8.40
CHEMBL429037 1 8.30
CHEMBL11706 BMS-248360 1 8.22
CHEMBL12592 1 8.15
CHEMBL275545 1 8.10
CHEMBL12779 1 8.10
CHEMBL275523 1 7.89
CHEMBL12557 1 7.85
CHEMBL12144 1 7.80
CHEMBL12590 1 7.80
CHEMBL12333 1 7.68
CHEMBL12172 1 7.64
CHEMBL417429 1 7.62
CHEMBL11528 1 7.52
CHEMBL12348 1 7.46
CHEMBL274154 1 7.40
CHEMBL12102 1 7.29
CHEMBL12703 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11840 Ki = 0.6 nM 9.22
CHEMBL12233 Ki = 1.3 nM 8.89
CHEMBL12588 Ki = 2.0 nM 8.70
CHEMBL12013 Ki = 2.0 nM 8.70
CHEMBL12106 Ki = 2.0 nM 8.70
CHEMBL12175 Ki = 3.0 nM 8.52
CHEMBL266628 Ki = 4.0 nM 8.40
CHEMBL268706 Ki = 4.0 nM 8.40
CHEMBL429037 Ki = 5.0 nM 8.30
CHEMBL11706 BMS-248360 Ki = 6.0 nM 8.22
CHEMBL12592 Ki = 7.0 nM 8.15
CHEMBL275545 Ki = 8.0 nM 8.10
CHEMBL12779 Ki = 8.0 nM 8.10
CHEMBL275523 Ki = 13.0 nM 7.89
CHEMBL12557 Ki = 14.0 nM 7.85
CHEMBL12144 Ki = 16.0 nM 7.80
CHEMBL12590 Ki = 16.0 nM 7.80
CHEMBL12333 Ki = 21.0 nM 7.68
CHEMBL12172 Ki = 23.0 nM 7.64
CHEMBL417429 Ki = 24.0 nM 7.62
CHEMBL11528 Ki = 30.0 nM 7.52
CHEMBL12348 Ki = 35.0 nM 7.46
CHEMBL274154 Ki = 40.0 nM 7.40
CHEMBL12102 Ki = 51.0 nM 7.29
CHEMBL12703 Ki = 360.0 nM 6.44