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Assay Detail

CHEMBL863398

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

Binding
Displacement of [125I]AB-MECA from human adenosine A3 receptor transfected in CHO cells
39
Total Activities
39
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 Expert

Target

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

Publication

Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.
Jeong LS, Lee HW, Jacobson KA, Kim HO, Shin DH, Lee JA, Gao ZG, Lu C, Duong HT, Gunaga P, Lee SK, Jin DZ, Chun MW, Moon HR.
J Med Chem (2006) 49 : 273 -281
PubMed 16392812 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 7.31 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201706 1 9.55
CHEMBL200732 1 9.42
CHEMBL203357 1 9.40
CHEMBL200705 1 9.17
CHEMBL200854 1 9.05
CHEMBL201427 1 8.96
CHEMBL201324 1 8.79
CHEMBL370187 1 8.66
CHEMBL200184 1 8.65
CHEMBL200099 1 8.60
CHEMBL199877 1 8.55
CHEMBL202189 1 8.55
CHEMBL370446 1 8.53
CHEMBL200279 1 8.44
CHEMBL381408 1 8.37
CHEMBL381868 1 8.26
CHEMBL200778 1 7.76
CHEMBL200407 1 7.74
CHEMBL200072 1 7.56
CHEMBL199541 1 7.53
CHEMBL200919 1 7.38
CHEMBL199307 1 7.07
CHEMBL199414 1 6.51
CHEMBL200339 1 6.46
CHEMBL200064 1 6.45
CHEMBL440215 1 6.38
CHEMBL199522 1 6.36
CHEMBL409142 1 6.29
CHEMBL371022 1 6.20
CHEMBL372602 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201706 Ki = 0.28 nM 9.55
CHEMBL200732 Ki = 0.38 nM 9.42
CHEMBL203357 Ki = 0.4 nM 9.40
CHEMBL200705 Ki = 0.67 nM 9.17
CHEMBL200854 Ki = 0.89 nM 9.05
CHEMBL201427 Ki = 1.1 nM 8.96
CHEMBL201324 Ki = 1.63 nM 8.79
CHEMBL370187 Ki = 2.18 nM 8.66
CHEMBL200184 Ki = 2.24 nM 8.65
CHEMBL200099 Ki = 2.5 nM 8.60
CHEMBL202189 Ki = 2.83 nM 8.55
CHEMBL199877 Ki = 2.82 nM 8.55
CHEMBL370446 Ki = 2.96 nM 8.53
CHEMBL200279 Ki = 3.64 nM 8.44
CHEMBL381408 Ki = 4.27 nM 8.37
CHEMBL381868 Ki = 5.56 nM 8.26
CHEMBL200778 Ki = 17.4 nM 7.76
CHEMBL200407 Ki = 18.2 nM 7.74
CHEMBL200072 Ki = 27.8 nM 7.56
CHEMBL199541 Ki = 29.7 nM 7.53
CHEMBL200919 Ki = 41.9 nM 7.38
CHEMBL199307 Ki = 85.6 nM 7.07
CHEMBL199414 Ki = 308.0 nM 6.51
CHEMBL200339 Ki = 343.0 nM 6.46
CHEMBL200064 Ki = 354.0 nM 6.45
CHEMBL440215 Ki = 415.0 nM 6.38
CHEMBL199522 Ki = 433.0 nM 6.36
CHEMBL409142 Ki = 510.0 nM 6.29
CHEMBL371022 Ki = 632.0 nM 6.20
CHEMBL372602 Ki = 878.0 nM 6.06
CHEMBL380773 Ki = 1440.0 nM 5.84
CHEMBL200033 Ki = 1500.0 nM 5.82
CHEMBL202923 Ki = 2700.0 nM 5.57
CHEMBL412259 Ki = 3500.0 nM 5.46
CHEMBL383283 Ki = 3870.0 nM 5.41
CHEMBL201934 Ki = 4020.0 nM 5.40
CHEMBL200332 Ki = 4440.0 nM 5.35
CHEMBL200372 Ki = 7670.0 nM 5.12
CHEMBL199413 Ki = 49200.0 nM 4.31