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Assay Detail

CHEMBL643130

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

Binding
Binding affinity against rat adenosine A3 receptor expressed in CHO cells using [125I]-.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists.
Baraldi PG, Cacciari B, Pineda de Las Infantas MJ, Romagnoli R, Spalluto G, Volpini R, Costanzi S, Vittori S, Cristalli G, Melman N, Park KS, Ji XD, Jacobson KA.
J Med Chem (1998) 41 : 3174 -3185
PubMed 9703463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 6.80 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL608327 1 9.48
CHEMBL119709 IB-MECA 1 8.96
CHEMBL265587 1 8.01
CHEMBL203933 1 7.79
CHEMBL204820 1 7.77
CHEMBL203812 1 7.68
CHEMBL426847 1 7.42
CHEMBL2113540 1 7.27
CHEMBL380914 1 7.11
CHEMBL203667 1 7.05
CHEMBL610394 1 6.97
CHEMBL464859 NECA 1 6.95
CHEMBL383268 1 6.83
CHEMBL610112 1 6.81
CHEMBL204190 1 6.81
CHEMBL383548 1 6.78
CHEMBL203958 1 6.78
CHEMBL413046 1 6.68
CHEMBL379472 1 6.60
CHEMBL437503 1 6.50
CHEMBL204246 1 6.50
CHEMBL203960 1 6.49
CHEMBL204651 1 6.39
CHEMBL2113550 1 6.39
CHEMBL202690 1 6.27
CHEMBL206265 1 6.24
CHEMBL381917 1 6.21
CHEMBL206116 1 6.16
CHEMBL377291 1 6.15
CHEMBL437506 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL608327 Ki = 0.33 nM 9.48
CHEMBL119709 IB-MECA Ki = 1.1 nM 8.96
CHEMBL265587 Ki = 9.73 nM 8.01
CHEMBL203933 Ki = 16.3 nM 7.79
CHEMBL204820 Ki = 17.1 nM 7.77
CHEMBL203812 Ki = 20.9 nM 7.68
CHEMBL426847 Ki = 38.3 nM 7.42
CHEMBL2113540 Ki = 54.1 nM 7.27
CHEMBL380914 Ki = 77.6 nM 7.11
CHEMBL203667 Ki = 89.5 nM 7.05
CHEMBL610394 Ki = 107.0 nM 6.97
CHEMBL464859 NECA Ki = 113.0 nM 6.95
CHEMBL383268 Ki = 149.0 nM 6.83
CHEMBL610112 Ki = 155.0 nM 6.81
CHEMBL204190 Ki = 154.0 nM 6.81
CHEMBL383548 Ki = 167.0 nM 6.78
CHEMBL203958 Ki = 168.0 nM 6.78
CHEMBL413046 Ki = 211.0 nM 6.68
CHEMBL379472 Ki = 251.0 nM 6.60
CHEMBL437503 Ki = 319.0 nM 6.50
CHEMBL204246 Ki = 315.0 nM 6.50
CHEMBL203960 Ki = 324.0 nM 6.49
CHEMBL204651 Ki = 411.0 nM 6.39
CHEMBL2113550 Ki = 405.0 nM 6.39
CHEMBL202690 Ki = 532.0 nM 6.27
CHEMBL206265 Ki = 581.0 nM 6.24
CHEMBL381917 Ki = 611.0 nM 6.21
CHEMBL206116 Ki = 696.0 nM 6.16
CHEMBL377291 Ki = 713.0 nM 6.15
CHEMBL437506 Ki = 754.0 nM 6.12
CHEMBL426669 Ki = 824.0 nM 6.08
CHEMBL205058 Ki = 837.0 nM 6.08
CHEMBL202722 Ki = 979.0 nM 6.01
CHEMBL437315 Ki = 5550.0 nM 5.26
CHEMBL202249 Ki = 5700.0 nM 5.24