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Assay Detail

CHEMBL636642

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

Binding
Inhibition of [3H]- PIA binding at adenosine A1 receptor on rat cerebral cortex membranes.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Xanthine functionalized congeners as potent ligands at A2-adenosine receptors.
Jacobson KA, Ukena D, Padgett W, Daly JW, Kirk KL.
J Med Chem (1987) 30 : 211 -214
PubMed 3806597 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.63 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70059 1 9.06
CHEMBL273094 XANTHINE AMINE CONGENER 1 8.92
CHEMBL16866 1 8.03
CHEMBL68756 1 8.03
CHEMBL305765 1 7.92
CHEMBL158507 1 7.89
CHEMBL66207 1 7.89
CHEMBL66523 1 7.89
CHEMBL17141 1 7.60
CHEMBL441598 1 7.57
CHEMBL70188 1 7.38
CHEMBL27041 1 7.30
CHEMBL67389 1 7.24
CHEMBL66053 1 7.24
CHEMBL11348 1 7.19
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 7.16
CHEMBL305212 1 7.05
CHEMBL307313 1 6.85
CHEMBL66919 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70059 Ki = 0.87 nM 9.06
CHEMBL273094 XANTHINE AMINE CONGENER Ki = 1.2 nM 8.92
CHEMBL16866 Ki = 9.3 nM 8.03
CHEMBL68756 Ki = 9.4 nM 8.03
CHEMBL305765 Ki = 12.0 nM 7.92
CHEMBL158507 Ki = 13.0 nM 7.89
CHEMBL66207 Ki = 13.0 nM 7.89
CHEMBL66523 Ki = 13.0 nM 7.89
CHEMBL17141 Ki = 25.0 nM 7.60
CHEMBL441598 Ki = 27.0 nM 7.57
CHEMBL70188 Ki = 42.0 nM 7.38
CHEMBL27041 Ki = 50.0 nM 7.30
CHEMBL67389 Ki = 58.0 nM 7.24
CHEMBL66053 Ki = 57.0 nM 7.24
CHEMBL11348 Ki = 65.0 nM 7.19
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 70.0 nM 7.16
CHEMBL305212 Ki = 90.0 nM 7.05
CHEMBL307313 Ki = 140.0 nM 6.85
CHEMBL66919 Ki = 180.0 nM 6.75