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Assay Detail

CHEMBL642194

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

Binding
Displacement of [3H]-R-PIA from adenosine A1 receptor of rat brain membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.
Jiang J, Li AH, Jang SY, Chang L, Melman N, Moro S, Ji X, Lobkovsky EB, Clardy JC, Jacobson KA.
J Med Chem (1999) 42 : 3055 -3065
PubMed 10447949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 4.92 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105672 1 6.11
CHEMBL315984 1 5.23
CHEMBL283013 1 5.18
CHEMBL315458 1 4.96
CHEMBL431232 1 4.79
CHEMBL103433 1 4.60
CHEMBL104198 1 4.50
CHEMBL321579 1 4.50
CHEMBL89852 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105672 Ki = 785.0 nM 6.11
CHEMBL315984 Ki = 5930.0 nM 5.23
CHEMBL283013 Ki = 6660.0 nM 5.18
CHEMBL315458 Ki = 11000.0 nM 4.96
CHEMBL431232 Ki = 16400.0 nM 4.79
CHEMBL103433 Ki = 25000.0 nM 4.60
CHEMBL104198 Ki = 32000.0 nM 4.50
CHEMBL321579 Ki = 32000.0 nM 4.50
CHEMBL89852 Ki = 40100.0 nM 4.40