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Assay Detail

CHEMBL648963

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

Binding
Inhibition of specific binding of [125I]angiotensin-II to angiotensin 1 receptor in rat lung membrane preparation
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Lung
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

6-Substituted benzimidazoles as new nonpeptide angiotensin II receptor antagonists: synthesis, biological activity, and structure-activity relationships.
Ries UJ, Mihm G, Narr B, Hasselbach KM, Wittneben H, Entzeroth M, van Meel JC, Wienen W, Hauel NH.
J Med Chem (1993) 36 : 4040 -4051
PubMed 8258826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.04 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1017 TELMISARTAN 4.0 1 8.52
CHEMBL130095 1 8.52
CHEMBL424629 1 8.52
CHEMBL130910 1 8.52
CHEMBL128922 1 8.40
CHEMBL129950 1 8.40
CHEMBL337232 1 8.30
CHEMBL131767 1 8.30
CHEMBL130746 1 8.10
CHEMBL132226 1 8.00
CHEMBL132282 1 7.96
CHEMBL338954 1 7.89
CHEMBL337025 1 7.68
CHEMBL130741 1 7.62
CHEMBL130896 1 7.58
CHEMBL131433 1 7.58
CHEMBL132280 1 7.48
CHEMBL131839 1 7.47
CHEMBL191 LOSARTAN 4.0 1 7.46
CHEMBL434640 1 7.09
CHEMBL128049 1 7.07
CHEMBL434815 1 6.80
CHEMBL130322 1 6.80
CHEMBL131209 1 6.80
CHEMBL334515 1 6.75
CHEMBL407978 1 6.62
CHEMBL274447 1 6.46
CHEMBL128340 1 6.41
CHEMBL7632 1 6.40
CHEMBL131365 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1017 TELMISARTAN IC50 = 3.0 nM 8.52
CHEMBL130095 IC50 = 3.0 nM 8.52
CHEMBL424629 IC50 = 3.0 nM 8.52
CHEMBL130910 IC50 = 3.0 nM 8.52
CHEMBL128922 IC50 = 4.0 nM 8.40
CHEMBL129950 IC50 = 4.0 nM 8.40
CHEMBL337232 IC50 = 5.0 nM 8.30
CHEMBL131767 IC50 = 5.0 nM 8.30
CHEMBL130746 IC50 = 8.0 nM 8.10
CHEMBL132226 IC50 = 10.0 nM 8.00
CHEMBL132282 IC50 = 11.0 nM 7.96
CHEMBL338954 IC50 = 13.0 nM 7.89
CHEMBL337025 IC50 = 21.0 nM 7.68
CHEMBL130741 IC50 = 24.0 nM 7.62
CHEMBL131433 IC50 = 26.0 nM 7.58
CHEMBL130896 IC50 = 26.0 nM 7.58
CHEMBL132280 IC50 = 33.0 nM 7.48
CHEMBL131839 IC50 = 34.0 nM 7.47
CHEMBL191 LOSARTAN IC50 = 35.0 nM 7.46
CHEMBL434640 IC50 = 81.0 nM 7.09
CHEMBL128049 IC50 = 86.0 nM 7.07
CHEMBL434815 IC50 = 160.0 nM 6.80
CHEMBL131209 IC50 = 160.0 nM 6.80
CHEMBL130322 IC50 = 158.0 nM 6.80
CHEMBL334515 IC50 = 180.0 nM 6.75
CHEMBL407978 IC50 = 240.0 nM 6.62
CHEMBL274447 IC50 = 350.0 nM 6.46
CHEMBL128340 IC50 = 390.0 nM 6.41
CHEMBL7632 IC50 = 400.0 nM 6.40
CHEMBL131365 IC50 = 460.0 nM 6.34
CHEMBL131948 IC50 = 480.0 nM 6.32
CHEMBL130828 IC50 = 540.0 nM 6.27
CHEMBL336130 IC50 = 800.0 nM 6.10
CHEMBL128318 IC50 = 820.0 nM 6.09
CHEMBL130600 IC50 = 850.0 nM 6.07
CHEMBL128913 IC50 = 1060.0 nM 5.97
CHEMBL130539 IC50 = 1200.0 nM 5.92
CHEMBL131722 IC50 = 1200.0 nM 5.92
CHEMBL339360 IC50 = 1700.0 nM 5.77
CHEMBL335734 IC50 = 1800.0 nM 5.75
CHEMBL334741 IC50 = 5700.0 nM 5.24
CHEMBL337269 IC50 = 29300.0 nM 4.53