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Assay Detail

CHEMBL772780

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

Functional
Inhibition of angiotensin II induced contractions in rabbit aortic ring preparation.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (CHEMBL2094256)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

1,3- And 1,5-bisbiphenylyl substituted 3-metcaptotriazoles as angiotensin II receptor antagonists
Bandurco V, Murray W, Gill A, Addo M, Lewis J, Wachter M, Hadden S, Underwood D, Cheung W
Bioorg Med Chem Lett (1993) 3 : 375 -379
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 21 6.92 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191 LOSARTAN 4.0 1 8.80
CHEMBL340315 1 8.40
CHEMBL215312 1 8.30
CHEMBL125831 1 8.10
CHEMBL341149 1 8.00
CHEMBL126051 1 7.50
CHEMBL410674 1 7.20
CHEMBL125432 1 7.00
CHEMBL122213 1 7.00
CHEMBL124213 1 6.70
CHEMBL121828 1 6.60
CHEMBL123549 1 6.50
CHEMBL341009 1 6.30
CHEMBL338760 1 6.10
CHEMBL123051 1 6.10
CHEMBL338761 1 5.90
CHEMBL122096 1 5.00
CHEMBL121710 1 5.00
CHEMBL126104 1 -
CHEMBL124626 1 -
CHEMBL263444 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191 LOSARTAN Kd = 1.585 nM 8.80
CHEMBL340315 Kd = 3.981 nM 8.40
CHEMBL215312 Kd = 5.012 nM 8.30
CHEMBL125831 Kd = 7.943 nM 8.10
CHEMBL341149 Kd = 10.0 nM 8.00
CHEMBL126051 Kd = 31.62 nM 7.50
CHEMBL410674 Kd = 63.1 nM 7.20
CHEMBL125432 Kd = 100.0 nM 7.00
CHEMBL122213 Kd = 100.0 nM 7.00
CHEMBL124213 Kd = 199.53 nM 6.70
CHEMBL121828 Kd = 251.19 nM 6.60
CHEMBL123549 Kd = 316.23 nM 6.50
CHEMBL341009 Kd = 501.19 nM 6.30
CHEMBL338760 Kd = 794.33 nM 6.10
CHEMBL123051 Kd = 794.33 nM 6.10
CHEMBL338761 Kd = 1258.93 nM 5.90
CHEMBL122096 Kd = 10000.0 nM 5.00
CHEMBL121710 Kd = 10000.0 nM 5.00
CHEMBL126104 Kd > 10000.0 nM -
CHEMBL124626 Kd > 10000.0 nM -
CHEMBL263444 Kd > 10000.0 nM -