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Assay Detail

CHEMBL873053

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

Binding
Binding affinity at Mutant (H272E) human adenosine A3 receptor expressed in COS-7 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS-7
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.
Jacobson KA, Gao ZG, Chen A, Barak D, Kim SA, Lee K, Link A, Rompaey PV, van Calenbergh S, Liang BT.
J Med Chem (2001) 44 : 4125 -4136
PubMed 11708915 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.01 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL133591 1 9.72
CHEMBL133566 1 8.68
CHEMBL439976 1 8.64
CHEMBL129903 1 8.02
CHEMBL133387 1 8.00
CHEMBL431733 NAMODENOSON 3.0 1 7.70
CHEMBL132629 1 7.50
CHEMBL340998 1 7.48
CHEMBL338352 1 7.12
CHEMBL133809 1 6.52
CHEMBL302376 1 6.37
CHEMBL128929 1 5.77
CHEMBL464859 NECA 1 5.50
CHEMBL16687 CGS-15943 1 5.49
CHEMBL285819 1 4.94
CHEMBL273094 XANTHINE AMINE CONGENER 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL133591 Ki = 0.19 nM 9.72
CHEMBL133566 Ki = 2.1 nM 8.68
CHEMBL439976 Ki = 2.3 nM 8.64
CHEMBL129903 Ki = 9.6 nM 8.02
CHEMBL133387 Ki = 9.9 nM 8.00
CHEMBL431733 NAMODENOSON Ki = 20.1 nM 7.70
CHEMBL132629 Ki = 32.0 nM 7.50
CHEMBL340998 Ki = 33.3 nM 7.48
CHEMBL338352 Ki = 75.0 nM 7.12
CHEMBL133809 Ki = 301.0 nM 6.52
CHEMBL302376 Ki = 425.0 nM 6.37
CHEMBL128929 Ki = 1690.0 nM 5.77
CHEMBL464859 NECA Ki = 3200.0 nM 5.50
CHEMBL16687 CGS-15943 Ki = 3260.0 nM 5.49
CHEMBL285819 Ki = 11600.0 nM 4.94
CHEMBL273094 XANTHINE AMINE CONGENER Ki = 20100.0 nM 4.70