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Assay Detail

CHEMBL2167688

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

Functional
Antagonist activity at human Adenosine receptor A1 assessed as inhibition of cAMP production
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and characterization of optimized adenosine A₂A/A₁ receptor antagonists for the treatment of Parkinson's disease.
Shook BC, Rassnick S, Wallace N, Crooke J, Ault M, Chakravarty D, Barbay JK, Wang A, Powell MT, Leonard K, Alford V, Scannevin RH, Carroll K, Lampron L, Westover L, Lim HK, Russell R, Branum S, Wells KM, Damon S, Youells S, Li X, Beauchamp DA, Rhodes K, Jackson PF.
J Med Chem (2012) 55 : 1402 -1417
PubMed 22239465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.98 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2165801 1 9.30
CHEMBL2165802 1 8.74
CHEMBL2165807 1 8.62
CHEMBL2165800 1 8.60
CHEMBL2165808 1 8.28
CHEMBL2165799 1 8.22
CHEMBL2165804 1 8.05
CHEMBL1087189 1 7.77
CHEMBL2165803 1 7.53
CHEMBL2165805 1 7.43
CHEMBL1095488 1 7.32
CHEMBL1087185 1 7.23
CHEMBL2165806 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2165801 Ki = 0.5 nM 9.30
CHEMBL2165802 Ki = 1.8 nM 8.74
CHEMBL2165807 Ki = 2.4 nM 8.62
CHEMBL2165800 Ki = 2.5 nM 8.60
CHEMBL2165808 Ki = 5.2 nM 8.28
CHEMBL2165799 Ki = 6.0 nM 8.22
CHEMBL2165804 Ki = 9.0 nM 8.05
CHEMBL1087189 Ki = 17.0 nM 7.77
CHEMBL2165803 Ki = 29.3 nM 7.53
CHEMBL2165805 Ki = 37.3 nM 7.43
CHEMBL1095488 Ki = 48.2 nM 7.32
CHEMBL1087185 Ki = 58.4 nM 7.23
CHEMBL2165806 Ki = 223.0 nM 6.65