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Assay Detail

CHEMBL899346

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

Binding
Displacement of [125I]SP from human NK1 receptor expressed in CHO cells in presence of 50% human serum
10
Total Activities
9
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 Intermediate

Target

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

Publication

Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
Young JR, Eid R, Turner C, DeVita RJ, Kurtz MM, Tsao KL, Chicchi GG, Wheeldon A, Carlson E, Mills SG.
Bioorg Med Chem Lett (2007) 17 : 5310 -5315
PubMed 17723300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.71 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392466 1 9.77
CHEMBL391964 1 9.68
CHEMBL391615 1 9.29
CHEMBL392463 1 8.55
CHEMBL391963 2 8.35
CHEMBL392465 1 8.22
CHEMBL235882 1 8.10
CHEMBL392464 1 7.70
CHEMBL237796 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392466 IC50 = 0.17 nM 9.77
CHEMBL391964 IC50 = 0.21 nM 9.68
CHEMBL391615 IC50 = 0.51 nM 9.29
CHEMBL392463 IC50 = 2.8 nM 8.55
CHEMBL391963 IC50 = 4.5 nM 8.35
CHEMBL392465 IC50 = 6.0 nM 8.22
CHEMBL235882 IC50 = 8.0 nM 8.10
CHEMBL392464 IC50 = 20.0 nM 7.70
CHEMBL391963 IC50 - -
CHEMBL237796 IC50 - -