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Assay Detail

CHEMBL648961

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

Binding
Binding affinity for rat angiotensin II receptor, type 1
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Type-1 angiotensin II receptor B (CHEMBL263)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, structural studies, biological evaluation, and computational simulations of novel potent AT(1) angiotensin II receptor antagonists based on the 4-phenylquinoline structure.
Cappelli A, Pericot Mohr Gl Gl, Gallelli A, Rizzo M, Anzini M, Vomero S, Mennuni L, Ferrari F, Makovec F, Menziani MC, De Benedetti PG, Giorgi G.
J Med Chem (2004) 47 : 2574 -2586
PubMed 15115399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.64 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7550 L-158809 1 9.40
CHEMBL408403 ANGIOTENSIN II 4.0 1 9.40
CHEMBL315104 1 9.10
CHEMBL296725 1 9.00
CHEMBL1069 VALSARTAN 4.0 1 8.72
CHEMBL47382 1 8.40
CHEMBL87327 1 8.38
CHEMBL85595 1 8.25
CHEMBL191 LOSARTAN 4.0 1 8.17
CHEMBL315022 1 8.17
CHEMBL86247 1 8.16
CHEMBL315021 FORASARTAN 2.0 1 8.16
CHEMBL314315 1 8.11
CHEMBL84573 1 8.05
CHEMBL87842 1 8.00
CHEMBL87779 1 7.96
CHEMBL315387 1 7.92
CHEMBL315165 1 7.89
CHEMBL86562 1 7.89
CHEMBL85405 1 7.89
CHEMBL86437 1 7.77
CHEMBL86346 1 7.75
CHEMBL86436 1 7.54
CHEMBL541212 1 7.48
CHEMBL423861 1 7.39
CHEMBL86655 1 7.28
CHEMBL47459 1 7.22
CHEMBL312889 1 7.18
CHEMBL87884 1 7.13
CHEMBL86344 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7550 L-158809 IC50 = 0.4 nM 9.40
CHEMBL408403 ANGIOTENSIN II IC50 = 0.4 nM 9.40
CHEMBL315104 IC50 = 0.8 nM 9.10
CHEMBL296725 IC50 = 1.0 nM 9.00
CHEMBL1069 VALSARTAN IC50 = 1.9 nM 8.72
CHEMBL47382 IC50 = 4.0 nM 8.40
CHEMBL87327 IC50 = 4.2 nM 8.38
CHEMBL85595 IC50 = 5.6 nM 8.25
CHEMBL191 LOSARTAN IC50 = 6.7 nM 8.17
CHEMBL315022 IC50 = 6.8 nM 8.17
CHEMBL86247 IC50 = 6.9 nM 8.16
CHEMBL315021 FORASARTAN IC50 = 6.9 nM 8.16
CHEMBL314315 IC50 = 7.7 nM 8.11
CHEMBL84573 IC50 = 9.0 nM 8.05
CHEMBL87842 IC50 = 10.0 nM 8.00
CHEMBL87779 IC50 = 11.0 nM 7.96
CHEMBL315387 IC50 = 12.0 nM 7.92
CHEMBL315165 IC50 = 13.0 nM 7.89
CHEMBL86562 IC50 = 13.0 nM 7.89
CHEMBL85405 IC50 = 13.0 nM 7.89
CHEMBL86437 IC50 = 17.0 nM 7.77
CHEMBL86346 IC50 = 18.0 nM 7.75
CHEMBL86436 IC50 = 29.0 nM 7.54
CHEMBL541212 IC50 = 33.0 nM 7.48
CHEMBL423861 IC50 = 41.0 nM 7.39
CHEMBL86655 IC50 = 52.0 nM 7.28
CHEMBL47459 IC50 = 60.0 nM 7.22
CHEMBL312889 IC50 = 66.0 nM 7.18
CHEMBL87884 IC50 = 74.0 nM 7.13
CHEMBL86344 IC50 = 98.0 nM 7.01
CHEMBL83414 IC50 = 106.0 nM 6.97
CHEMBL88067 IC50 = 110.0 nM 6.96
CHEMBL410939 IC50 = 116.0 nM 6.94
CHEMBL87411 IC50 = 150.0 nM 6.82
CHEMBL437659 IC50 = 215.0 nM 6.67
CHEMBL87655 IC50 = 250.0 nM 6.60
CHEMBL314807 IC50 = 261.0 nM 6.58
CHEMBL87694 IC50 = 326.0 nM 6.49
CHEMBL83452 IC50 = 492.0 nM 6.31
CHEMBL313718 IC50 = 576.0 nM 6.24
CHEMBL88081 IC50 = 819.0 nM 6.09
CHEMBL87997 IC50 > 300.0 nM -