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Assay Detail

CHEMBL3055839

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

Binding
Antagonist activity at angiotensin 2 type-1 receptor in Oryctolagus cuniculus (rabbit) aorta in presence of bovine serum albumin
110
Total Activities
55
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL3948)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Structural insights for 3H-1, -2, -4 triazolinones as angiotensin II receptor antagonists using QSAR techniques
Parate A, Chaturvedi SC
Med Chem Res (2010) 19 : 375 -391
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
logIC50 55 - -
IC50 55 7.95 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419483 2 9.13
CHEMBL87074 2 9.07
CHEMBL312913 2 9.03
CHEMBL19018 2 8.92
CHEMBL431411 2 8.85
CHEMBL87964 2 8.74
CHEMBL87513 2 8.70
CHEMBL18287 2 8.62
CHEMBL87239 2 8.54
CHEMBL87778 2 8.54
CHEMBL313025 2 8.49
CHEMBL87057 2 8.49
CHEMBL315776 2 8.44
CHEMBL83180 2 8.39
CHEMBL422593 2 8.34
CHEMBL85545 2 8.31
CHEMBL84627 2 8.30
CHEMBL314042 2 8.25
CHEMBL278741 2 8.24
CHEMBL316052 2 8.24
CHEMBL85765 2 8.22
CHEMBL83248 2 8.18
CHEMBL87985 2 8.11
CHEMBL313579 2 8.11
CHEMBL82797 2 8.09
CHEMBL87392 2 8.02
CHEMBL86084 2 8.00
CHEMBL407827 2 7.96
CHEMBL314447 2 7.96
CHEMBL312921 2 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419483 IC50 = 0.74 nM 9.13
CHEMBL87074 IC50 = 0.85 nM 9.07
CHEMBL312913 IC50 = 0.93 nM 9.03
CHEMBL19018 IC50 = 1.2 nM 8.92
CHEMBL431411 IC50 = 1.4 nM 8.85
CHEMBL87964 IC50 = 1.8 nM 8.74
CHEMBL87513 IC50 = 2.0 nM 8.70
CHEMBL18287 IC50 = 2.4 nM 8.62
CHEMBL87778 IC50 = 2.9 nM 8.54
CHEMBL87239 IC50 = 2.9 nM 8.54
CHEMBL313025 IC50 = 3.2 nM 8.49
CHEMBL87057 IC50 = 3.2 nM 8.49
CHEMBL315776 IC50 = 3.6 nM 8.44
CHEMBL83180 IC50 = 4.1 nM 8.39
CHEMBL422593 IC50 = 4.6 nM 8.34
CHEMBL85545 IC50 = 4.9 nM 8.31
CHEMBL84627 IC50 = 5.0 nM 8.30
CHEMBL314042 IC50 = 5.6 nM 8.25
CHEMBL278741 IC50 = 5.8 nM 8.24
CHEMBL316052 IC50 = 5.7 nM 8.24
CHEMBL85765 IC50 = 6.0 nM 8.22
CHEMBL83248 IC50 = 6.6 nM 8.18
CHEMBL313579 IC50 = 7.7 nM 8.11
CHEMBL87985 IC50 = 7.7 nM 8.11
CHEMBL82797 IC50 = 8.2 nM 8.09
CHEMBL87392 IC50 = 9.5 nM 8.02
CHEMBL86084 IC50 = 10.0 nM 8.00
CHEMBL407827 IC50 = 11.0 nM 7.96
CHEMBL314447 IC50 = 11.0 nM 7.96
CHEMBL312921 IC50 = 11.0 nM 7.96
CHEMBL87129 IC50 = 12.0 nM 7.92
CHEMBL87798 IC50 = 12.0 nM 7.92
CHEMBL315128 IC50 = 14.0 nM 7.85
CHEMBL86255 IC50 = 15.0 nM 7.82
CHEMBL86906 IC50 = 16.0 nM 7.80
CHEMBL85541 IC50 = 17.0 nM 7.77
CHEMBL314179 IC50 = 17.0 nM 7.77
CHEMBL315615 IC50 = 18.0 nM 7.75
CHEMBL85596 IC50 = 21.0 nM 7.68
CHEMBL85876 IC50 = 22.0 nM 7.66
CHEMBL87885 IC50 = 23.0 nM 7.64
CHEMBL86613 IC50 = 27.0 nM 7.57
CHEMBL87073 IC50 = 33.0 nM 7.48
CHEMBL420970 IC50 = 43.0 nM 7.37
CHEMBL69508 IC50 = 60.0 nM 7.22
CHEMBL86143 IC50 = 68.0 nM 7.17
CHEMBL86440 IC50 = 69.0 nM 7.16
CHEMBL313017 IC50 = 70.0 nM 7.16
CHEMBL84630 IC50 = 80.0 nM 7.10
CHEMBL86741 IC50 = 79.0 nM 7.10