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Assay Detail

CHEMBL636667

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

Binding
Displacement of [3H]CHA from Adenosine A1 receptor of rat brain
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2-[N'-(3-arylallylidene)hydrazino]adenosines showing A2a adenosine agonist properties and vasodilation activity.
Viziano M, Ongini E, Conti A, Zocchi C, Seminati M, Pocar D.
J Med Chem (1995) 38 : 3581 -3585
PubMed 7658444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.58 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284969 1 8.89
CHEMBL464859 NECA 1 7.98
CHEMBL2113552 1 7.19
CHEMBL2113553 1 7.00
CHEMBL2113554 1 6.58
CHEMBL2113560 1 6.37
CHEMBL2113556 1 6.28
CHEMBL2113559 1 6.26
CHEMBL331372 CGS-21680 1 6.25
CHEMBL2113558 1 6.03
CHEMBL2113563 1 5.98
CHEMBL2113555 1 5.78
CHEMBL611571 1 5.75
CHEMBL2113564 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284969 Ki = 1.3 nM 8.89
CHEMBL464859 NECA Ki = 10.4 nM 7.98
CHEMBL2113552 Ki = 64.0 nM 7.19
CHEMBL2113553 Ki = 101.0 nM 7.00
CHEMBL2113554 Ki = 264.0 nM 6.58
CHEMBL2113560 Ki = 425.0 nM 6.37
CHEMBL2113556 Ki = 524.0 nM 6.28
CHEMBL2113559 Ki = 545.0 nM 6.26
CHEMBL331372 CGS-21680 Ki = 569.0 nM 6.25
CHEMBL2113558 Ki = 935.0 nM 6.03
CHEMBL2113563 Ki = 1050.0 nM 5.98
CHEMBL2113555 Ki = 1670.0 nM 5.78
CHEMBL611571 Ki = 1770.0 nM 5.75
CHEMBL2113564 Ki = 1850.0 nM 5.73