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Assay Detail

CHEMBL643602

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

Binding
In vitro inhibition of specific binding of [125 I] A II to rat liver membrane.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Pyrido[2,3-d]pyrimidine angiotensin II antagonists.
Ellingboe JW, Antane M, Nguyen TT, Collini MD, Antane S, Bender R, Hartupee D, White V, McCallum J, Park CH.
J Med Chem (1994) 37 : 542 -550
PubMed 8120871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.86 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL150507 1 8.89
CHEMBL153188 1 8.87
CHEMBL152957 1 8.74
CHEMBL348472 1 8.66
CHEMBL152958 1 8.64
CHEMBL440731 1 8.52
CHEMBL345528 1 8.49
CHEMBL432162 TASOSARTAN 2.0 1 8.28
CHEMBL153472 1 7.89
CHEMBL346420 1 7.64
CHEMBL155163 1 7.61
CHEMBL347320 1 7.61
CHEMBL191 LOSARTAN 4.0 1 7.46
CHEMBL433930 1 7.31
CHEMBL421969 1 7.29
CHEMBL150987 1 7.07
CHEMBL357998 1 7.02
CHEMBL153092 1 6.77
CHEMBL153499 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL150507 IC50 = 1.3 nM 8.89
CHEMBL153188 IC50 = 1.35 nM 8.87
CHEMBL152957 IC50 = 1.8 nM 8.74
CHEMBL348472 IC50 = 2.2 nM 8.66
CHEMBL152958 IC50 = 2.3 nM 8.64
CHEMBL440731 IC50 = 3.0 nM 8.52
CHEMBL345528 IC50 = 3.2 nM 8.49
CHEMBL432162 TASOSARTAN IC50 = 5.2 nM 8.28
CHEMBL153472 IC50 = 13.0 nM 7.89
CHEMBL346420 IC50 = 23.0 nM 7.64
CHEMBL155163 IC50 = 24.3 nM 7.61
CHEMBL347320 IC50 = 24.6 nM 7.61
CHEMBL191 LOSARTAN IC50 = 34.7 nM 7.46
CHEMBL433930 IC50 = 49.4 nM 7.31
CHEMBL421969 IC50 = 50.7 nM 7.29
CHEMBL150987 IC50 = 85.0 nM 7.07
CHEMBL357998 IC50 = 94.9 nM 7.02
CHEMBL153092 IC50 = 170.0 nM 6.77
CHEMBL153499 IC50 = 285.0 nM 6.54