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Assay Detail

CHEMBL644579

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Binding
Activity against high affinity Angiotensin II receptor, type 1 was measured from the ability to inhibit [125I]angiotensin II binding to rat uterine membrane.
15
Total Activities
15
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

Nonpeptide angiotensin II antagonists: N-phenyl-1H-pyrrole derivatives are angiotensin II receptor antagonists.
Bovy PR, Reitz DB, Collins JT, Chamberlain TS, Olins GM, Corpus VM, McMahon EG, Palomo MA, Koepke JP, Smits GJ.
J Med Chem (1993) 36 : 101 -110
PubMed 8421274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.54 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85595 1 8.19
CHEMBL12810 1 7.48
CHEMBL276150 1 7.28
CHEMBL12693 1 7.14
CHEMBL12451 1 7.06
CHEMBL12766 1 7.02
CHEMBL12737 1 6.57
CHEMBL276381 1 6.54
CHEMBL12548 1 6.32
CHEMBL267547 1 5.96
CHEMBL13071 1 5.70
CHEMBL430279 1 5.38
CHEMBL191 LOSARTAN 4.0 1 4.44
CHEMBL12190 1 -
CHEMBL274447 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85595 IC50 = 6.5 nM 8.19
CHEMBL12810 IC50 = 33.0 nM 7.48
CHEMBL276150 IC50 = 52.0 nM 7.28
CHEMBL12693 IC50 = 72.0 nM 7.14
CHEMBL12451 IC50 = 88.0 nM 7.06
CHEMBL12766 IC50 = 95.0 nM 7.02
CHEMBL12737 IC50 = 270.0 nM 6.57
CHEMBL276381 IC50 = 290.0 nM 6.54
CHEMBL12548 IC50 = 480.0 nM 6.32
CHEMBL267547 IC50 = 1100.0 nM 5.96
CHEMBL13071 IC50 = 2000.0 nM 5.70
CHEMBL430279 IC50 = 4200.0 nM 5.38
CHEMBL191 LOSARTAN IC50 = 36000.0 nM 4.44
CHEMBL12190 IC50 = 870000.0 nM -
CHEMBL274447 IC50 = 170000.0 nM -