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Assay Detail

CHEMBL1785218

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

Binding
Displacement of [3H]SP from human recombinant NK1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist.
Ballet S, Feytens D, Buysse K, Chung NN, Lemieux C, Tumati S, Keresztes A, Van Duppen J, Lai J, Varga E, Porreca F, Schiller PW, Vanden Broeck J, Tourwé D.
J Med Chem (2011) 54 : 2467 -2476
PubMed 21413804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.70 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782141 1 9.30
CHEMBL1782139 1 7.57
CHEMBL1782137 1 7.50
CHEMBL1782138 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782141 Ki = 0.5 nM 9.30
CHEMBL1782139 Ki = 27.0 nM 7.57
CHEMBL1782137 Ki = 32.0 nM 7.50
CHEMBL1782138 Ki = 387.0 nM 6.41