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Assay Detail

CHEMBL829700

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

Binding
Displacement of [125I]-Ang II from pig uterus membrane angiotensin II type 2 (AT2) receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-2 angiotensin II receptor (CHEMBL4607)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.
Wan Y, Wallinder C, Plouffe B, Beaudry H, Mahalingam AK, Wu X, Johansson B, Holm M, Botoros M, Karlén A, Pettersson A, Nyberg F, Fändriks L, Gallo-Payet N, Hallberg A, Alterman M.
J Med Chem (2004) 47 : 5995 -6008
PubMed 15537354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.49 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL189568 BULOXIBUTID 0.5 1 9.40
CHEMBL361927 1 9.30
CHEMBL288174 1 8.55
CHEMBL190577 1 8.49
CHEMBL366210 1 8.40
CHEMBL190811 1 8.15
CHEMBL191468 1 7.16
CHEMBL187871 1 -
CHEMBL370939 1 -
CHEMBL190796 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL189568 BULOXIBUTID Ki = 0.4 nM 9.40
CHEMBL361927 Ki = 0.5 nM 9.30
CHEMBL288174 Ki = 2.8 nM 8.55
CHEMBL190577 Ki = 3.2 nM 8.49
CHEMBL366210 Ki = 4.0 nM 8.40
CHEMBL190811 Ki = 7.1 nM 8.15
CHEMBL191468 Ki = 70.0 nM 7.16
CHEMBL187871 Ki > 10000.0 nM -
CHEMBL370939 Ki > 10000.0 nM -
CHEMBL190796 Ki > 10000.0 nM -