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Assay Detail

CHEMBL644805

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Binding
Ability to inhibit the binding of [3H]N6-phenylisopropyl adenosine to adenosine receptor in rat cerebral cortex membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Adenosine receptor (CHEMBL2111386)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Binary drugs: conjugates of purines and a peptide that bind to both adenosine and substance P receptors.
Jacobson KA, Lipkowski AW, Moody TW, Padgett W, Pijl E, Kirk KL, Daly JW.
J Med Chem (1987) 30 : 1529 -1532
PubMed 2441057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.90 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39503 1 8.92
CHEMBL37306 1 8.68
CHEMBL37351 1 8.37
CHEMBL606297 1 7.80
CHEMBL3144091 1 7.80
CHEMBL3143947 1 7.52
CHEMBL3143946 1 7.46
CHEMBL605246 1 6.68
CHEMBL2372353 1 -
CHEMBL2372385 1 -
CHEMBL235363 SUBSTANCE P 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39503 Ki = 1.2 nM 8.92
CHEMBL37306 Ki = 2.1 nM 8.68
CHEMBL37351 Ki = 4.3 nM 8.37
CHEMBL606297 Ki = 16.0 nM 7.80
CHEMBL3144091 Ki = 16.0 nM 7.80
CHEMBL3143947 Ki = 30.0 nM 7.52
CHEMBL3143946 Ki = 35.0 nM 7.46
CHEMBL605246 Ki = 210.0 nM 6.68
CHEMBL2372353 Ki > 30000.0 nM -
CHEMBL2372385 Ki > 30000.0 nM -
CHEMBL235363 SUBSTANCE P Ki > 30000.0 nM -