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Assay Detail

CHEMBL643131

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

Binding
Binding affinity for rat A3-adenosine receptor expressed in chinese hamster ovarian cells (assayed by the displacement of specific [125I]-N6-(4-amino-3-iodobenzyl)-adenosine-5''-N-methyluronamide)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type ovarian
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.
Gallo-Rodriguez C, Ji XD, Melman N, Siegman BD, Sanders LH, Orlina J, Fischer B, Pu Q, Olah ME, van Galen PJ.
J Med Chem (1994) 37 : 636 -646
PubMed 8126704 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.63 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119709 IB-MECA 1 8.96
CHEMBL133566 1 8.90
CHEMBL2113620 1 8.72
CHEMBL610426 1 8.55
CHEMBL1256785 1 8.00
CHEMBL609642 1 7.92
CHEMBL609245 1 7.85
CHEMBL609923 1 7.77
CHEMBL2113639 1 7.75
CHEMBL610143 1 7.72
CHEMBL609830 1 7.55
CHEMBL608762 1 7.51
CHEMBL610996 1 7.38
CHEMBL608653 1 6.31
CHEMBL610429 1 5.88
CHEMBL608652 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119709 IB-MECA Ki = 1.1 nM 8.96
CHEMBL133566 Ki = 1.27 nM 8.90
CHEMBL2113620 Ki = 1.9 nM 8.72
CHEMBL610426 Ki = 2.8 nM 8.55
CHEMBL1256785 Ki = 10.0 nM 8.00
CHEMBL609642 Ki = 12.0 nM 7.92
CHEMBL609245 Ki = 14.0 nM 7.85
CHEMBL609923 Ki = 17.0 nM 7.77
CHEMBL2113639 Ki = 18.0 nM 7.75
CHEMBL610143 Ki = 19.0 nM 7.72
CHEMBL609830 Ki = 28.0 nM 7.55
CHEMBL608762 Ki = 31.0 nM 7.51
CHEMBL610996 Ki = 41.4 nM 7.38
CHEMBL608653 Ki = 494.0 nM 6.31
CHEMBL610429 Ki = 1310.0 nM 5.88
CHEMBL608652 Ki = 4500.0 nM 5.35