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Assay Detail

CHEMBL3108367

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

Binding
Displacement of [125I]-Bolton Hunter-Substance P from human NK1 receptor
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Substance-P receptor (CHEMBL249)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.
Hanessian S, Babonneau V, Boyer N, Mannoury la Cour C, Millan MJ, De Nanteuil G.
Bioorg Med Chem Lett (2014) 24 : 510 -514
PubMed 24374277 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.66 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3104784 1 7.90
CHEMBL3104786 1 7.80
CHEMBL3104778 1 7.10
CHEMBL3104782 1 7.00
CHEMBL3104780 1 6.60
CHEMBL3104774 1 6.60
CHEMBL3104777 1 6.50
CHEMBL3104775 1 6.50
CHEMBL3104773 1 6.10
CHEMBL3104776 1 5.60
CHEMBL3104781 1 5.60
CHEMBL3104768 1 -
CHEMBL3104779 1 -
CHEMBL3104772 1 -
CHEMBL3104771 1 -
CHEMBL3104770 1 -
CHEMBL3104769 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3104784 Ki = 12.59 nM 7.90
CHEMBL3104786 Ki = 15.85 nM 7.80
CHEMBL3104778 Ki = 79.43 nM 7.10
CHEMBL3104782 Ki = 100.0 nM 7.00
CHEMBL3104780 Ki = 251.19 nM 6.60
CHEMBL3104774 Ki = 251.19 nM 6.60
CHEMBL3104777 Ki = 316.23 nM 6.50
CHEMBL3104775 Ki = 316.23 nM 6.50
CHEMBL3104773 Ki = 794.33 nM 6.10
CHEMBL3104776 Ki = 2511.89 nM 5.60
CHEMBL3104781 Ki = 2511.89 nM 5.60
CHEMBL3104768 Ki > 100000.0 nM -
CHEMBL3104779 Ki > 10000.0 nM -
CHEMBL3104772 Ki > 10000.0 nM -
CHEMBL3104771 Ki > 10000.0 nM -
CHEMBL3104770 Ki > 10000.0 nM -
CHEMBL3104769 Ki > 10000.0 nM -