Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1768168

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

Binding
Displacement of [125I]BH-SP from human recombinant NK1 receptor expressed in CHO cells after 90 mins
23
Total Activities
23
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

Non-peptide NK1 receptor ligands based on the 4-phenylpyridine moiety.
Giuliani G, Cappelli A, Matarrese M, Masiello V, Turolla EA, Monterisi C, Fazio F, Anzini M, Pericot Mohr G, Riitano D, Finetti F, Morbidelli L, Ziche M, Giorgi G, Vomero S.
Bioorg Med Chem (2011) 19 : 2242 -2251
PubMed 21421318 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.05 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235363 SUBSTANCE P 1.0 1 8.82
CHEMBL1765500 1 8.32
CHEMBL281491 1 7.72
CHEMBL1765494 1 7.50
CHEMBL1765502 1 7.39
CHEMBL25639 1 7.38
CHEMBL1765499 1 7.28
CHEMBL1765498 1 7.28
CHEMBL1765506 1 7.28
CHEMBL1765504 1 7.24
CHEMBL413027 1 7.04
CHEMBL1765496 1 7.04
CHEMBL1765492 1 7.01
CHEMBL24894 1 6.68
CHEMBL277004 1 6.64
CHEMBL1765497 1 6.63
CHEMBL282853 1 6.59
CHEMBL1765495 1 6.57
CHEMBL1765503 1 6.55
CHEMBL1765493 1 6.47
CHEMBL1765501 1 6.36
CHEMBL1765491 1 6.18
CHEMBL1765505 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235363 SUBSTANCE P IC50 = 1.5 nM 8.82
CHEMBL1765500 IC50 = 4.8 nM 8.32
CHEMBL281491 IC50 = 19.0 nM 7.72
CHEMBL1765494 IC50 = 32.0 nM 7.50
CHEMBL1765502 IC50 = 41.0 nM 7.39
CHEMBL25639 IC50 = 42.0 nM 7.38
CHEMBL1765499 IC50 = 53.0 nM 7.28
CHEMBL1765498 IC50 = 52.0 nM 7.28
CHEMBL1765506 IC50 = 53.0 nM 7.28
CHEMBL1765504 IC50 = 57.0 nM 7.24
CHEMBL413027 IC50 = 92.0 nM 7.04
CHEMBL1765496 IC50 = 91.0 nM 7.04
CHEMBL1765492 IC50 = 98.0 nM 7.01
CHEMBL24894 IC50 = 208.0 nM 6.68
CHEMBL277004 IC50 = 227.0 nM 6.64
CHEMBL1765497 IC50 = 235.0 nM 6.63
CHEMBL282853 IC50 = 257.0 nM 6.59
CHEMBL1765495 IC50 = 270.0 nM 6.57
CHEMBL1765503 IC50 = 279.0 nM 6.55
CHEMBL1765493 IC50 = 342.0 nM 6.47
CHEMBL1765501 IC50 = 434.0 nM 6.36
CHEMBL1765491 IC50 = 653.0 nM 6.18
CHEMBL1765505 IC50 = 698.0 nM 6.16