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Assay Detail

CHEMBL648844

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

Binding
Displacement of [125I]-Sar1-Ile8-A II at the rabbit aorta angiotensin II receptor, type 1
98
Total Activities
98
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.
Ashton WT, Cantone CL, Chang LL, Hutchins SM, Strelitz RA, MacCoss M, Chang RS, Lotti VJ, Faust KA, Chen TB.
J Med Chem (1993) 36 : 591 -609
PubMed 8496939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 98 7.16 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7550 L-158809 1 9.52
CHEMBL352236 1 8.85
CHEMBL157577 1 8.82
CHEMBL345459 1 8.52
CHEMBL345570 1 8.48
CHEMBL156934 1 8.39
CHEMBL907 CARBOXYLIC ACID METABOLITE 1 8.22
CHEMBL347404 1 8.21
CHEMBL346542 1 8.18
CHEMBL155877 1 8.17
CHEMBL347135 1 8.17
CHEMBL345717 1 8.15
CHEMBL158133 1 8.13
CHEMBL345139 1 8.12
CHEMBL345404 1 8.11
CHEMBL434844 1 8.05
CHEMBL348143 1 8.00
CHEMBL155638 1 7.96
CHEMBL157980 1 7.89
CHEMBL156084 1 7.85
CHEMBL155948 1 7.85
CHEMBL155661 1 7.82
CHEMBL352235 1 7.82
CHEMBL422333 1 7.77
CHEMBL157690 1 7.70
CHEMBL157524 1 7.68
CHEMBL155008 1 7.62
CHEMBL347392 1 7.62
CHEMBL157620 1 7.58
CHEMBL157779 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7550 L-158809 IC50 = 0.3 nM 9.52
CHEMBL352236 IC50 = 1.4 nM 8.85
CHEMBL157577 IC50 = 1.5 nM 8.82
CHEMBL345459 IC50 = 3.0 nM 8.52
CHEMBL345570 IC50 = 3.3 nM 8.48
CHEMBL156934 IC50 = 4.1 nM 8.39
CHEMBL907 CARBOXYLIC ACID METABOLITE IC50 = 6.0 nM 8.22
CHEMBL347404 IC50 = 6.1 nM 8.21
CHEMBL346542 IC50 = 6.6 nM 8.18
CHEMBL155877 IC50 = 6.8 nM 8.17
CHEMBL347135 IC50 = 6.8 nM 8.17
CHEMBL345717 IC50 = 7.1 nM 8.15
CHEMBL158133 IC50 = 7.4 nM 8.13
CHEMBL345139 IC50 = 7.6 nM 8.12
CHEMBL345404 IC50 = 7.8 nM 8.11
CHEMBL434844 IC50 = 8.9 nM 8.05
CHEMBL348143 IC50 = 10.0 nM 8.00
CHEMBL155638 IC50 = 11.0 nM 7.96
CHEMBL157980 IC50 = 13.0 nM 7.89
CHEMBL156084 IC50 = 14.0 nM 7.85
CHEMBL155948 IC50 = 14.0 nM 7.85
CHEMBL155661 IC50 = 15.0 nM 7.82
CHEMBL352235 IC50 = 15.0 nM 7.82
CHEMBL422333 IC50 = 17.0 nM 7.77
CHEMBL157690 IC50 = 20.0 nM 7.70
CHEMBL157524 IC50 = 21.0 nM 7.68
CHEMBL347392 IC50 = 24.0 nM 7.62
CHEMBL155008 IC50 = 24.0 nM 7.62
CHEMBL157620 IC50 = 26.0 nM 7.58
CHEMBL157779 IC50 = 28.0 nM 7.55
CHEMBL155554 IC50 = 28.0 nM 7.55
CHEMBL158257 IC50 = 30.0 nM 7.52
CHEMBL423233 IC50 = 30.0 nM 7.52
CHEMBL157878 IC50 = 30.0 nM 7.52
CHEMBL348606 IC50 = 31.0 nM 7.51
CHEMBL155984 IC50 = 32.0 nM 7.50
CHEMBL154027 IC50 = 33.0 nM 7.48
CHEMBL155035 IC50 = 35.0 nM 7.46
CHEMBL158267 IC50 = 36.0 nM 7.44
CHEMBL346145 IC50 = 36.0 nM 7.44
CHEMBL158115 IC50 = 40.0 nM 7.40
CHEMBL157185 IC50 = 42.0 nM 7.38
CHEMBL347630 IC50 = 48.0 nM 7.32
CHEMBL348568 IC50 = 49.0 nM 7.31
CHEMBL191 LOSARTAN IC50 = 50.0 nM 7.30
CHEMBL345826 IC50 = 50.0 nM 7.30
CHEMBL350241 IC50 = 55.0 nM 7.26
CHEMBL155305 IC50 = 55.0 nM 7.26
CHEMBL157512 IC50 = 57.0 nM 7.24
CHEMBL153968 IC50 = 60.0 nM 7.22