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Assay Detail

CHEMBL649536

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

Binding
Binding affinity at Angiotensin II receptor, type 1 in rat liver membranes by [125I]-Ang II displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo.
Wan Y, Wallinder C, Johansson B, Holm M, Mahalingam AK, Wu X, Botros M, Karlén A, Pettersson A, Nyberg F, Fändriks L, Hallberg A, Alterman M.
J Med Chem (2004) 47 : 1536 -1546
PubMed 14998339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.80 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288174 1 8.41
CHEMBL289306 1 7.47
CHEMBL39132 1 7.46
CHEMBL40563 1 7.26
CHEMBL290370 1 7.21
CHEMBL415875 1 6.96
CHEMBL291089 1 6.92
CHEMBL432095 1 6.73
CHEMBL291124 1 6.64
CHEMBL290708 1 6.61
CHEMBL289211 1 6.47
CHEMBL409843 1 6.46
CHEMBL289775 1 6.39
CHEMBL291125 1 6.34
CHEMBL287829 1 6.16
CHEMBL289803 1 6.14
CHEMBL38842 1 5.98
CHEMBL277388 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288174 Ki = 3.9 nM 8.41
CHEMBL289306 Ki = 34.0 nM 7.47
CHEMBL39132 Ki = 34.9 nM 7.46
CHEMBL40563 Ki = 55.2 nM 7.26
CHEMBL290370 Ki = 62.0 nM 7.21
CHEMBL415875 Ki = 109.0 nM 6.96
CHEMBL291089 Ki = 121.0 nM 6.92
CHEMBL432095 Ki = 185.0 nM 6.73
CHEMBL291124 Ki = 231.0 nM 6.64
CHEMBL290708 Ki = 248.0 nM 6.61
CHEMBL289211 Ki = 339.0 nM 6.47
CHEMBL409843 Ki = 343.0 nM 6.46
CHEMBL289775 Ki = 410.0 nM 6.39
CHEMBL291125 Ki = 455.0 nM 6.34
CHEMBL287829 Ki = 693.0 nM 6.16
CHEMBL289803 Ki = 728.0 nM 6.14
CHEMBL38842 Ki = 1038.0 nM 5.98
CHEMBL277388 Ki > 10000.0 nM -