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Assay Detail

CHEMBL807902

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

Binding
Binding affinity against Gln165Ala mutant type human Tachykinin receptor 1 expressed in CHO cells was measured by its ability to displace [125I]- Tyr-8 substance P.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and biological evaluation of NK1 antagonists derived from L-tryptophan.
MacLeod AM, Cascieri MA, Merchant KJ, Sadowski S, Hardwicke S, Lewis RT, MacIntyre DE, Metzger JM, Fong TM, Shepheard S.
J Med Chem (1995) 38 : 934 -941
PubMed 7535362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.85 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420543 1 8.85
CHEMBL173231 1 8.40
CHEMBL174038 1 8.10
CHEMBL22870 L-732138 1 8.09
CHEMBL173396 1 8.00
CHEMBL120781 1 8.00
CHEMBL16192 CP-96345 1 7.66
CHEMBL367034 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420543 IC50 = 1.4 nM 8.85
CHEMBL173231 IC50 = 4.0 nM 8.40
CHEMBL174038 IC50 = 8.0 nM 8.10
CHEMBL22870 L-732138 IC50 = 8.1 nM 8.09
CHEMBL173396 IC50 = 10.0 nM 8.00
CHEMBL120781 IC50 = 10.0 nM 8.00
CHEMBL16192 CP-96345 IC50 = 22.0 nM 7.66
CHEMBL367034 IC50 = 2100.0 nM 5.68