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Assay Detail

CHEMBL2044692

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Functional
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and pharmacological evaluation of dual acting antioxidant A(2A) adenosine receptor agonists.
Hausler NE, Devine SM, McRobb FM, Warfe L, Pouton CW, Haynes JM, Bottle SE, White PJ, Scammells PJ.
J Med Chem (2012) 55 : 3521 -3534
PubMed 22432713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.70 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2042311 1 8.15
CHEMBL2042304 1 8.10
CHEMBL2042297 1 7.64
CHEMBL2042306 1 7.48
CHEMBL2042298 1 6.98
CHEMBL2042310 1 6.95
CHEMBL2042303 1 6.92
CHEMBL2042305 1 6.92
CHEMBL2042299 1 6.85
CHEMBL2042307 1 6.83
CHEMBL2042300 1 6.59
CHEMBL2042302 1 6.12
CHEMBL2042308 1 5.86
CHEMBL2042309 1 5.85
CHEMBL2042312 1 5.76
CHEMBL2042301 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2042311 IC50 = 7.04 nM 8.15
CHEMBL2042304 IC50 = 8.0 nM 8.10
CHEMBL2042297 IC50 = 23.0 nM 7.64
CHEMBL2042306 IC50 = 33.0 nM 7.48
CHEMBL2042298 IC50 = 104.0 nM 6.98
CHEMBL2042310 IC50 = 113.0 nM 6.95
CHEMBL2042303 IC50 = 121.0 nM 6.92
CHEMBL2042305 IC50 = 120.0 nM 6.92
CHEMBL2042299 IC50 = 141.0 nM 6.85
CHEMBL2042307 IC50 = 149.0 nM 6.83
CHEMBL2042300 IC50 = 259.0 nM 6.59
CHEMBL2042302 IC50 = 756.0 nM 6.12
CHEMBL2042308 IC50 = 1390.0 nM 5.86
CHEMBL2042309 IC50 = 1407.0 nM 5.85
CHEMBL2042312 IC50 = 1721.0 nM 5.76
CHEMBL2042301 IC50 = 60097.0 nM 4.22