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Assay Detail

CHEMBL1100567

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

Binding
Displacement of [125I][Sar1,Ile8]Ang2 from human AT1 receptor N111G constitutively active mutant expressed in CHO cells by gamma counting
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The amino-terminus of angiotensin II contacts several ectodomains of the angiotensin II receptor AT1.
Fillion D, Lemieux G, Basambombo LL, Lavigne P, Guillemette G, Leduc R, Escher E.
J Med Chem (2010) 53 : 2063 -2075
PubMed 20146480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.86 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1076604 1 9.52
CHEMBL1076602 1 9.40
CHEMBL1076603 1 9.40
CHEMBL408403 ANGIOTENSIN II 4.0 1 9.30
CHEMBL1076663 1 9.30
CHEMBL1076632 1 9.22
CHEMBL1076601 1 9.22
CHEMBL1076613 1 9.15
CHEMBL1076633 1 9.15
CHEMBL1076662 1 9.15
CHEMBL1076612 1 9.10
CHEMBL1076631 1 8.42
CHEMBL1076630 1 7.89
CHEMBL1076664 1 7.50
CHEMBL1076629 1 7.24
CHEMBL1076661 1 -
CHEMBL1076605 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1076604 Ki = 0.3 nM 9.52
CHEMBL1076602 Ki = 0.4 nM 9.40
CHEMBL1076603 Ki = 0.4 nM 9.40
CHEMBL408403 ANGIOTENSIN II Ki = 0.5 nM 9.30
CHEMBL1076663 Ki = 0.5 nM 9.30
CHEMBL1076632 Ki = 0.6 nM 9.22
CHEMBL1076601 Ki = 0.6 nM 9.22
CHEMBL1076613 Ki = 0.7 nM 9.15
CHEMBL1076633 Ki = 0.7 nM 9.15
CHEMBL1076662 Ki = 0.7 nM 9.15
CHEMBL1076612 Ki = 0.8 nM 9.10
CHEMBL1076631 Ki = 3.8 nM 8.42
CHEMBL1076630 Ki = 12.8 nM 7.89
CHEMBL1076664 Ki = 31.6 nM 7.50
CHEMBL1076629 Ki = 58.2 nM 7.24
CHEMBL1076661 Ki >= 250.0 nM -
CHEMBL1076605 Ki >= 250.0 nM -