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Assay Detail

CHEMBL646365

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

Binding
Binding affinity at Adenosine A2 receptor from rat striatal membranes by N-[3H] ethyladenosin-5'- uronamide displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
Suzuki F, Shimada J, Shiozaki S, Ichikawa S, Ishii A, Nakamura J, Nonaka H, Kobayashi H, Fuse E.
J Med Chem (1993) 36 : 2508 -2518
PubMed 8355252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.23 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27508 1 8.11
CHEMBL27203 1 7.75
CHEMBL120350 1 6.60
CHEMBL116486 1 6.54
CHEMBL84144 1 6.48
CHEMBL312352 1 6.48
CHEMBL82589 1 6.42
CHEMBL313780 1 6.39
CHEMBL84363 1 6.37
CHEMBL310557 1 6.37
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.23
CHEMBL82417 1 5.70
CHEMBL84545 1 5.57
CHEMBL418101 1 5.29
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.80
CHEMBL113 CAFFEINE 4.0 1 4.57
CHEMBL312857 1 -
CHEMBL83822 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27508 Ki = 7.8 nM 8.11
CHEMBL27203 Ki = 18.0 nM 7.75
CHEMBL120350 Ki = 250.0 nM 6.60
CHEMBL116486 Ki = 290.0 nM 6.54
CHEMBL84144 Ki = 330.0 nM 6.48
CHEMBL312352 Ki = 330.0 nM 6.48
CHEMBL82589 Ki = 380.0 nM 6.42
CHEMBL313780 Ki = 410.0 nM 6.39
CHEMBL84363 Ki = 430.0 nM 6.37
CHEMBL310557 Ki = 430.0 nM 6.37
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 590.0 nM 6.23
CHEMBL82417 Ki = 2000.0 nM 5.70
CHEMBL84545 Ki = 2700.0 nM 5.57
CHEMBL418101 Ki = 5100.0 nM 5.29
CHEMBL1355736 THEOPHYLLINE Ki = 16000.0 nM 4.80
CHEMBL113 CAFFEINE Ki = 27000.0 nM 4.57
CHEMBL312857 Ki > 100000.0 nM -
CHEMBL83822 Ki > 100000.0 nM -