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Assay Detail

CHEMBL802840

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

Binding
Ability to inhibit the binding of [125I]physalaemin to the SP receptors in rat telencephalon slices
11
Total Activities
11
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

Substance-P receptor (CHEMBL4027)
Type SINGLE PROTEIN
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 6.86 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235363 SUBSTANCE P 1.0 1 8.96
CHEMBL2371916 1 6.75
CHEMBL3143946 1 6.52
CHEMBL2372339 1 6.35
CHEMBL3144091 1 5.70
CHEMBL606297 1 -
CHEMBL3143947 1 -
CHEMBL2372353 1 -
CHEMBL2372385 1 -
CHEMBL39503 1 -
CHEMBL37306 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235363 SUBSTANCE P Ki = 1.1 nM 8.96
CHEMBL2371916 Ki = 180.0 nM 6.75
CHEMBL3143946 Ki = 300.0 nM 6.52
CHEMBL2372339 Ki = 450.0 nM 6.35
CHEMBL3144091 Ki = 2000.0 nM 5.70
CHEMBL606297 Ki > 10000.0 nM -
CHEMBL3143947 Ki > 10000.0 nM -
CHEMBL2372353 Ki > 10000.0 nM -
CHEMBL2372385 Ki > 10000.0 nM -
CHEMBL39503 Ki > 10000.0 nM -
CHEMBL37306 Ki > 10000.0 nM -