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Assay Detail

CHEMBL653127

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Binding
Inhibitory concentration that gave 50 percent displacement of specific binding of [3H]AII (2 nM) to Angiotensin II receptor
ChEMBL ↗
69
Total Activities
68
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 (CHEMBL2094112) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

The discovery of potent nonpeptide angiotensin II receptor antagonists: a new class of potent antihypertensives.
Duncia JV, Chiu AT, Carini DJ, Gregory GB, Johnson AL, Price WA, Wells GJ, Wong PC, Calabrese JC, Timmermans PB.
J Med Chem (1990) 33 : 1312 -1329
PubMed 2329553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 69 5.44 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284425 — — 1 7.92
CHEMBL1744348 — — 1 7.75
CHEMBL281589 — — 1 7.50
CHEMBL276956 — — 1 7.38
CHEMBL25031 — — 1 7.10
CHEMBL262958 — — 1 6.85
CHEMBL282491 — — 1 6.72
CHEMBL28011 — — 1 6.72
CHEMBL24364 — — 1 6.55
CHEMBL283071 — — 1 6.42
CHEMBL27725 — — 1 6.40
CHEMBL27839 — — 1 6.38
CHEMBL24512 — — 1 6.30
CHEMBL28391 — — 1 6.30
CHEMBL280868 — — 1 6.24
CHEMBL24934 — — 1 6.10
CHEMBL286028 — — 1 6.09
CHEMBL281514 — — 1 5.96
CHEMBL282283 — — 1 5.92
CHEMBL26727 — — 1 5.89
CHEMBL25686 — — 1 5.80
CHEMBL416384 — — 1 5.77
CHEMBL283983 — — 1 5.68
CHEMBL26712 — — 1 5.64
CHEMBL26673 — — 1 5.57
CHEMBL26765 — — 1 5.55
CHEMBL280193 — — 1 5.51
CHEMBL27977 — — 1 5.47
CHEMBL281068 — — 1 5.42
CHEMBL282307 — — 2 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284425 — IC50 = 12.0 nM 7.92
CHEMBL1744348 — IC50 = 18.0 nM 7.75
CHEMBL281589 — IC50 = 32.0 nM 7.50
CHEMBL276956 — IC50 = 42.0 nM 7.38
CHEMBL25031 — IC50 = 80.0 nM 7.10
CHEMBL262958 — IC50 = 140.0 nM 6.85
CHEMBL282491 — IC50 = 190.0 nM 6.72
CHEMBL28011 — IC50 = 190.0 nM 6.72
CHEMBL24364 — IC50 = 280.0 nM 6.55
CHEMBL283071 — IC50 = 380.0 nM 6.42
CHEMBL27725 — IC50 = 400.0 nM 6.40
CHEMBL27839 — IC50 = 420.0 nM 6.38
CHEMBL24512 — IC50 = 500.0 nM 6.30
CHEMBL28391 — IC50 = 500.0 nM 6.30
CHEMBL280868 — IC50 = 570.0 nM 6.24
CHEMBL24934 — IC50 = 790.0 nM 6.10
CHEMBL286028 — IC50 = 810.0 nM 6.09
CHEMBL281514 — IC50 = 1100.0 nM 5.96
CHEMBL282283 — IC50 = 1200.0 nM 5.92
CHEMBL26727 — IC50 = 1300.0 nM 5.89
CHEMBL25686 — IC50 = 1600.0 nM 5.80
CHEMBL416384 — IC50 = 1700.0 nM 5.77
CHEMBL283983 — IC50 = 2100.0 nM 5.68
CHEMBL26712 — IC50 = 2300.0 nM 5.64
CHEMBL26673 — IC50 = 2700.0 nM 5.57
CHEMBL26765 — IC50 = 2800.0 nM 5.55
CHEMBL280193 — IC50 = 3100.0 nM 5.51
CHEMBL27977 — IC50 = 3400.0 nM 5.47
CHEMBL281068 — IC50 = 3800.0 nM 5.42
CHEMBL282307 — IC50 = 3900.0 nM 5.41
CHEMBL282307 — IC50 = 4500.0 nM 5.35
CHEMBL27454 — IC50 = 5300.0 nM 5.28
CHEMBL281761 — IC50 = 5800.0 nM 5.24
CHEMBL25677 — IC50 = 5700.0 nM 5.24
CHEMBL26935 — IC50 = 5900.0 nM 5.23
CHEMBL25171 — IC50 = 6100.0 nM 5.21
CHEMBL28013 — IC50 = 6400.0 nM 5.19
CHEMBL28425 — IC50 = 6900.0 nM 5.16
CHEMBL282090 — IC50 = 7500.0 nM 5.12
CHEMBL27401 — IC50 = 8000.0 nM 5.10
CHEMBL280768 — IC50 = 11000.0 nM 4.96
CHEMBL279747 — IC50 = 11000.0 nM 4.96
CHEMBL284426 — IC50 = 13000.0 nM 4.89
CHEMBL24952 — IC50 = 15000.0 nM 4.82
CHEMBL25694 — IC50 = 19000.0 nM 4.72
CHEMBL431697 — IC50 = 22000.0 nM 4.66
CHEMBL25555 — IC50 = 27000.0 nM 4.57
CHEMBL24849 — IC50 = 28000.0 nM 4.55
CHEMBL25574 — IC50 = 32000.0 nM 4.50
CHEMBL27321 — IC50 = 38000.0 nM 4.42