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Assay Detail

CHEMBL829121

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

Binding
Inhibition of [125I]AB-MECA binding to rat Adenosine A3 receptor expressed in CHO cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A3 (CHEMBL3360)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
Tchilibon S, Joshi BV, Kim SK, Duong HT, Gao ZG, Jacobson KA.
J Med Chem (2005) 48 : 1745 -1758
PubMed 15771421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.96 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431733 NAMODENOSON 3.0 1 9.48
CHEMBL2368455 1 9.12
CHEMBL2112157 1 9.06
CHEMBL175543 1 9.00
CHEMBL27376 1 8.96
CHEMBL119709 IB-MECA 1 8.96
CHEMBL2112155 1 8.80
CHEMBL2112162 1 8.80
CHEMBL307199 1 8.57
CHEMBL2368367 1 8.41
CHEMBL66393 1 8.02
CHEMBL2368366 1 8.00
CHEMBL2368369 1 7.96
CHEMBL193385 1 7.46
CHEMBL331382 METRIFUDIL 2.0 1 7.42
CHEMBL283057 1 6.80
CHEMBL364671 1 6.54
CHEMBL193421 1 6.40
CHEMBL193692 1 6.27
CHEMBL383144 1 5.19
CHEMBL194830 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431733 NAMODENOSON Ki = 0.33 nM 9.48
CHEMBL2368455 Ki = 0.76 nM 9.12
CHEMBL2112157 Ki = 0.87 nM 9.06
CHEMBL175543 Ki = 1.0 nM 9.00
CHEMBL27376 Ki = 1.1 nM 8.96
CHEMBL119709 IB-MECA Ki = 1.1 nM 8.96
CHEMBL2112155 Ki = 1.6 nM 8.80
CHEMBL2112162 Ki = 1.6 nM 8.80
CHEMBL307199 Ki = 2.7 nM 8.57
CHEMBL2368367 Ki = 3.9 nM 8.41
CHEMBL66393 Ki = 9.5 nM 8.02
CHEMBL2368366 Ki = 10.0 nM 8.00
CHEMBL2368369 Ki = 11.0 nM 7.96
CHEMBL193385 Ki = 35.0 nM 7.46
CHEMBL331382 METRIFUDIL Ki = 38.0 nM 7.42
CHEMBL283057 Ki = 160.0 nM 6.80
CHEMBL364671 Ki = 290.0 nM 6.54
CHEMBL193421 Ki = 400.0 nM 6.40
CHEMBL193692 Ki = 540.0 nM 6.27
CHEMBL383144 Ki = 6400.0 nM 5.19
CHEMBL194830 Ki > 10000.0 nM -