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Assay Detail

CHEMBL982628

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

Binding
Displacement of [3H]CGS21680 form human adenosine A3 receptor expressed in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.
Melman A, Wang B, Joshi BV, Gao ZG, Castro Sd, Heller CL, Kim SK, Jeong LS, Jacobson KA.
Bioorg Med Chem (2008) 16 : 8546 -8556
PubMed 18752961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.16 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175543 1 9.54
CHEMBL490606 1 9.14
CHEMBL523797 1 8.97
CHEMBL489795 1 8.89
CHEMBL431733 NAMODENOSON 3.0 1 8.85
CHEMBL490607 1 8.85
CHEMBL490605 1 8.84
CHEMBL27376 1 8.82
CHEMBL353319 1 8.82
CHEMBL490405 1 8.80
CHEMBL522434 1 8.39
CHEMBL489175 1 7.91
CHEMBL373065 1 7.54
CHEMBL521621 1 7.15
CHEMBL491416 1 7.06
CHEMBL490403 1 6.71
CHEMBL491616 1 6.51
CHEMBL522111 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175543 Ki = 0.29 nM 9.54
CHEMBL490606 Ki = 0.73 nM 9.14
CHEMBL523797 Ki = 1.06 nM 8.97
CHEMBL489795 Ki = 1.3 nM 8.89
CHEMBL431733 NAMODENOSON Ki = 1.4 nM 8.85
CHEMBL490607 Ki = 1.42 nM 8.85
CHEMBL490605 Ki = 1.44 nM 8.84
CHEMBL27376 Ki = 1.5 nM 8.82
CHEMBL353319 Ki = 1.5 nM 8.82
CHEMBL490405 Ki = 1.58 nM 8.80
CHEMBL522434 Ki = 4.06 nM 8.39
CHEMBL489175 Ki = 12.4 nM 7.91
CHEMBL373065 Ki = 29.0 nM 7.54
CHEMBL521621 Ki = 70.2 nM 7.15
CHEMBL491416 Ki = 86.2 nM 7.06
CHEMBL490403 Ki = 196.0 nM 6.71
CHEMBL491616 Ki = 310.0 nM 6.51
CHEMBL522111 Ki = 1010.0 nM 6.00