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Assay Detail

CHEMBL767386

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

Functional
Tested in vitro for angiotensin II induced antagonistic activity in rabbit aorta, expressed as pA2
17
Total Activities
17
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

5-Membered ring heterocyclic carboxylic acids as angiotensin II antagonists
Pratt J, Jae H, Rosenberg S, Spina K, Winn M, Buckner S, Novosad E, Kerkman D, Shiosaki K, Opgenorth T, DeBernardis H
Bioorg Med Chem Lett (1994) 4 : 169 -172
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 17 8.17 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45927 1 9.29
CHEMBL298002 1 9.00
CHEMBL45998 1 8.86
CHEMBL46004 1 8.80
CHEMBL45911 1 8.63
CHEMBL47825 1 8.60
CHEMBL301132 1 8.36
CHEMBL301756 1 8.20
CHEMBL295817 1 7.94
CHEMBL298900 1 7.87
CHEMBL300191 1 7.56
CHEMBL297654 1 7.43
CHEMBL443521 1 7.34
CHEMBL296130 1 6.46
CHEMBL49579 1 -
CHEMBL48870 1 -
CHEMBL50773 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45927 Kd = 0.5129 nM 9.29
CHEMBL298002 Kd = 1.0 nM 9.00
CHEMBL45998 Kd = 1.38 nM 8.86
CHEMBL46004 Kd = 1.585 nM 8.80
CHEMBL45911 Kd = 2.344 nM 8.63
CHEMBL47825 Kd = 2.512 nM 8.60
CHEMBL301132 Kd = 4.365 nM 8.36
CHEMBL301756 Kd = 6.31 nM 8.20
CHEMBL295817 Kd = 11.48 nM 7.94
CHEMBL298900 Kd = 13.49 nM 7.87
CHEMBL300191 Kd = 27.54 nM 7.56
CHEMBL297654 Kd = 37.15 nM 7.43
CHEMBL443521 Kd = 45.71 nM 7.34
CHEMBL296130 Kd = 346.74 nM 6.46
CHEMBL49579 Kd > 100.0 nM -
CHEMBL48870 Kd > 1000.0 nM -
CHEMBL50773 Kd > 1000.0 nM -