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Assay Detail

CHEMBL643798

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

Binding
In vitro binding affinity determined by its ability to displace the specific binding ligand [125I]-Sar1, Ile8-AII from AT2 receptor in rat midbrain membranes
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Type-2 angiotensin II receptor (CHEMBL257)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Imidazo[4,5-b]pyridine-based AT1 / AT2 angiotensin II receptor antagonists
Mantlo NB, Kim D, Ondeyka D, Chang RS, Kivlighn SD, Siegl PK, Greenlee WJ
Bioorg Med Chem Lett (1994) 4 : 17 -22
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.10 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304946 1 9.60
CHEMBL304947 1 9.51
CHEMBL68618 1 9.35
CHEMBL306407 1 9.33
CHEMBL302102 1 9.15
CHEMBL302519 1 9.03
CHEMBL71388 1 8.65
CHEMBL67801 1 8.57
CHEMBL308237 1 8.41
CHEMBL67805 1 8.38
CHEMBL67921 1 8.25
CHEMBL68786 1 7.76
CHEMBL306641 1 7.55
CHEMBL68638 1 7.48
CHEMBL308238 1 7.23
CHEMBL71925 1 6.85
CHEMBL307757 1 6.40
CHEMBL448476 1 6.29
CHEMBL71253 1 6.05
CHEMBL7550 L-158809 1 -
CHEMBL296725 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304946 IC50 = 0.25 nM 9.60
CHEMBL304947 IC50 = 0.31 nM 9.51
CHEMBL68618 IC50 = 0.45 nM 9.35
CHEMBL306407 IC50 = 0.47 nM 9.33
CHEMBL302102 IC50 = 0.7 nM 9.15
CHEMBL302519 IC50 = 0.94 nM 9.03
CHEMBL71388 IC50 = 2.23 nM 8.65
CHEMBL67801 IC50 = 2.7 nM 8.57
CHEMBL308237 IC50 = 3.9 nM 8.41
CHEMBL67805 IC50 = 4.2 nM 8.38
CHEMBL67921 IC50 = 5.6 nM 8.25
CHEMBL68786 IC50 = 17.5 nM 7.76
CHEMBL306641 IC50 = 28.0 nM 7.55
CHEMBL68638 IC50 = 33.0 nM 7.48
CHEMBL308238 IC50 = 59.0 nM 7.23
CHEMBL71925 IC50 = 140.0 nM 6.85
CHEMBL307757 IC50 = 400.0 nM 6.40
CHEMBL448476 IC50 = 510.0 nM 6.29
CHEMBL71253 IC50 = 900.0 nM 6.05
CHEMBL7550 L-158809 IC50 > 10000.0 nM -
CHEMBL296725 IC50 > 10000.0 nM -