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Assay Detail

CHEMBL3768050

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

Binding
Displacement of 125I-[Sar1,Leu8] angiotensin-2 from rat type 1 angiotensin-2 receptor expressed in African green monkey COS7 cells after 24 hrs
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type COS-7
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.
Sallander J, Wallinder C, Hallberg A, Åqvist J, Gutiérrez-de-Terán H.
Bioorg Med Chem Lett (2016) 26 : 1355 -1359
PubMed 26810314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.81 9.77
IC50 3 8.47 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1016 CANDESARTAN 3.0 1 9.77
CHEMBL938 SARALASIN 4.0 1 9.66
CHEMBL404594 1 9.19
CHEMBL408403 ANGIOTENSIN II 4.0 1 9.02
CHEMBL39959 1 8.82
CHEMBL289614 1 8.68
CHEMBL191 LOSARTAN 4.0 1 7.92
CHEMBL34124 OLODANRIGAN 2.0 1 6.39
CHEMBL189568 BULOXIBUTID 0.5 1 -
CHEMBL2086892 1 -
CHEMBL217673 1 -
CHEMBL3394207 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1016 CANDESARTAN Ki = 0.17 nM 9.77
CHEMBL938 SARALASIN Ki = 0.22 nM 9.66
CHEMBL404594 Ki = 0.65 nM 9.19
CHEMBL408403 ANGIOTENSIN II Ki = 0.95 nM 9.02
CHEMBL39959 IC50 = 1.5 nM 8.82
CHEMBL289614 IC50 = 2.1 nM 8.68
CHEMBL191 LOSARTAN IC50 = 12.1 nM 7.92
CHEMBL34124 OLODANRIGAN Ki = 409.0 nM 6.39
CHEMBL189568 BULOXIBUTID Ki > 10000.0 nM -
CHEMBL2086892 Ki > 10000.0 nM -
CHEMBL217673 Ki > 10000.0 nM -
CHEMBL3394207 Ki > 10000.0 nM -