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Assay Detail

CHEMBL982624

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

Binding
Displacement of [3H]CCPA form human adenosine A1 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 A1 (CHEMBL226)
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 5.94 6.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27376 1 6.87
CHEMBL431733 NAMODENOSON 3.0 1 6.65
CHEMBL353319 1 6.62
CHEMBL521621 1 6.60
CHEMBL175543 1 6.58
CHEMBL491416 1 6.06
CHEMBL490403 1 6.00
CHEMBL522434 1 5.96
CHEMBL490607 1 5.95
CHEMBL489175 1 5.80
CHEMBL489795 1 5.75
CHEMBL490606 1 5.75
CHEMBL490605 1 5.52
CHEMBL490405 1 5.52
CHEMBL523797 1 5.51
CHEMBL491616 1 5.32
CHEMBL373065 1 5.23
CHEMBL522111 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27376 Ki = 136.0 nM 6.87
CHEMBL431733 NAMODENOSON Ki = 222.0 nM 6.65
CHEMBL353319 Ki = 240.0 nM 6.62
CHEMBL521621 Ki = 252.0 nM 6.60
CHEMBL175543 Ki = 260.0 nM 6.58
CHEMBL491416 Ki = 870.0 nM 6.06
CHEMBL490403 Ki = 1010.0 nM 6.00
CHEMBL522434 Ki = 1110.0 nM 5.96
CHEMBL490607 Ki = 1120.0 nM 5.95
CHEMBL489175 Ki = 1600.0 nM 5.80
CHEMBL489795 Ki = 1790.0 nM 5.75
CHEMBL490606 Ki = 1760.0 nM 5.75
CHEMBL490605 Ki = 3040.0 nM 5.52
CHEMBL490405 Ki = 3000.0 nM 5.52
CHEMBL523797 Ki = 3070.0 nM 5.51
CHEMBL491616 Ki = 4820.0 nM 5.32
CHEMBL373065 Ki = 5870.0 nM 5.23
CHEMBL522111 Ki = 6630.0 nM 5.18