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Assay Detail

CHEMBL645214

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

Binding
Binding affinity against Adenosine A1 receptor from guinea pig forebrain membranes by N6-[3H]- cyclohexyladenosine displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL2304404)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 19 7.60 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL82589 1 8.89
CHEMBL312857 1 8.62
CHEMBL116486 1 8.57
CHEMBL84363 1 8.52
CHEMBL84144 1 8.46
CHEMBL310557 1 8.25
CHEMBL312352 1 8.24
CHEMBL82417 1 8.21
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 8.19
CHEMBL292904 1 8.18
CHEMBL313780 1 7.92
CHEMBL418101 1 7.89
CHEMBL84545 1 7.82
CHEMBL83822 1 7.64
CHEMBL120350 1 6.92
CHEMBL27508 1 5.82
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.64
CHEMBL113 CAFFEINE 4.0 1 4.00
CHEMBL27203 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL82589 Ki = 1.3 nM 8.89
CHEMBL312857 Ki = 2.4 nM 8.62
CHEMBL116486 Ki = 2.7 nM 8.57
CHEMBL84363 Ki = 3.0 nM 8.52
CHEMBL84144 Ki = 3.5 nM 8.46
CHEMBL310557 Ki = 5.6 nM 8.25
CHEMBL312352 Ki = 5.7 nM 8.24
CHEMBL82417 Ki = 6.1 nM 8.21
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 6.4 nM 8.19
CHEMBL292904 Ki = 6.6 nM 8.18
CHEMBL313780 Ki = 12.0 nM 7.92
CHEMBL418101 Ki = 13.0 nM 7.89
CHEMBL84545 Ki = 15.0 nM 7.82
CHEMBL83822 Ki = 23.0 nM 7.64
CHEMBL120350 Ki = 120.0 nM 6.92
CHEMBL27508 Ki = 1500.0 nM 5.82
CHEMBL1355736 THEOPHYLLINE Ki = 23000.0 nM 4.64
CHEMBL113 CAFFEINE Ki = 100000.0 nM 4.00
CHEMBL27203 Ki > 100000.0 nM -