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Assay Detail

CHEMBL641986

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

Functional
Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor)
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL2605)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

1,3-Dialkyl-8-(p-sulfophenyl)xanthines: potent water-soluble antagonists for A1- and A2-adenosine receptors.
Daly JW, Padgett W, Shamim MT, Butts-Lamb P, Waters J.
J Med Chem (1985) 28 : 487 -492
PubMed 2984420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 5.78 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27155 1 7.30
CHEMBL423239 1 6.96
CHEMBL276830 1 6.89
CHEMBL27047 1 6.89
CHEMBL158507 1 6.52
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 6.26
CHEMBL418333 1 6.15
CHEMBL11033 1 6.05
CHEMBL11054 1 6.00
CHEMBL273671 1 6.00
CHEMBL11120 1 5.77
CHEMBL415248 1 5.77
CHEMBL11048 1 5.60
CHEMBL157655 1 5.57
CHEMBL8488 1 5.20
CHEMBL279688 1 5.16
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.85
CHEMBL89062 1 4.85
CHEMBL273953 1 4.82
CHEMBL21053 1 4.57
CHEMBL113 CAFFEINE 4.0 1 4.30
CHEMBL11146 1 -
CHEMBL20613 1 -
CHEMBL20402 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27155 Ki = 50.0 nM 7.30
CHEMBL423239 Ki = 110.0 nM 6.96
CHEMBL276830 Ki = 130.0 nM 6.89
CHEMBL27047 Ki = 130.0 nM 6.89
CHEMBL158507 Ki = 300.0 nM 6.52
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 550.0 nM 6.26
CHEMBL418333 Ki = 710.0 nM 6.15
CHEMBL11033 Ki = 900.0 nM 6.05
CHEMBL11054 Ki = 1000.0 nM 6.00
CHEMBL273671 Ki = 1000.0 nM 6.00
CHEMBL11120 Ki = 1700.0 nM 5.77
CHEMBL415248 Ki = 1700.0 nM 5.77
CHEMBL11048 Ki = 2500.0 nM 5.60
CHEMBL157655 Ki = 2700.0 nM 5.57
CHEMBL8488 Ki = 6300.0 nM 5.20
CHEMBL279688 Ki = 7000.0 nM 5.16
CHEMBL1355736 THEOPHYLLINE Ki = 14000.0 nM 4.85
CHEMBL89062 Ki = 14000.0 nM 4.85
CHEMBL273953 Ki = 15000.0 nM 4.82
CHEMBL21053 Ki = 27000.0 nM 4.57
CHEMBL113 CAFFEINE Ki = 50000.0 nM 4.30
CHEMBL11146 Ki > 30000.0 nM -
CHEMBL20613 Ki > 150000.0 nM -
CHEMBL20402 Ki > 10000.0 nM -