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Assay Detail

CHEMBL1785222

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Functional
Antagonist activity at NK1 receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous 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
IC50 2 8.69 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441225 CP-99994 1 9.77
CHEMBL120844 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441225 CP-99994 IC50 = 0.17 nM 9.77
CHEMBL120844 IC50 = 25.0 nM 7.60