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Assay Detail

CHEMBL4480627

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

Binding
Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes by radioligand competition assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membranes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Methoxy substituted 2-benzylidene-1-indanone derivatives as A1 and/or A2A AR antagonists for the potential treatment of neurological conditions.
Janse van Rensburg HD, Legoabe LJ, Terre'Blanche G, Van der Walt MM.
Medchemcomm (2019) 10 : 300 -309
PubMed 30881617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.71 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 9.40
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 8.17
CHEMBL4572336 1 7.39
CHEMBL4523006 1 7.38
CHEMBL4547939 1 6.36
CHEMBL4527335 1 6.02
CHEMBL4535634 1 5.79
CHEMBL4541726 1 5.78
CHEMBL4580228 1 5.48
CHEMBL4559281 1 5.37
CHEMBL4569263 1 -
CHEMBL4570432 1 -
CHEMBL4577288 1 -
CHEMBL3902894 1 -
CHEMBL1906073 1 -
CHEMBL28855 1 -
CHEMBL4552783 1 -
CHEMBL4572298 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 0.4 nM 9.40
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 6.8 nM 8.17
CHEMBL4572336 Ki = 41.0 nM 7.39
CHEMBL4523006 Ki = 42.0 nM 7.38
CHEMBL4547939 Ki = 435.0 nM 6.36
CHEMBL4527335 Ki = 956.0 nM 6.02
CHEMBL4535634 Ki = 1620.0 nM 5.79
CHEMBL4541726 Ki = 1650.0 nM 5.78
CHEMBL4580228 Ki = 3280.0 nM 5.48
CHEMBL4559281 Ki = 4290.0 nM 5.37
CHEMBL4569263 Ki > 100000.0 nM -
CHEMBL4570432 Ki > 100000.0 nM -
CHEMBL4577288 Ki > 100000.0 nM -
CHEMBL3902894 Ki > 100000.0 nM -
CHEMBL1906073 Ki > 100000.0 nM -
CHEMBL28855 Ki > 100000.0 nM -
CHEMBL4552783 Ki > 100000.0 nM -
CHEMBL4572298 Ki > 100000.0 nM -