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Assay Detail

CHEMBL700070

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

Binding
Inhibition of [3H]diltiazem binding to L-type [Ca2+] channel in rabbit skeletal muscle
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Muscle tissue
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

2(S)-((3,5-bis(trifluoromethyl)benzyl)-oxy)-3(S)-phenyl-4- ((3-oxo-1,2,4-triazol-5-yl)methyl)morpholine (1): a potent, orally active, morpholine-based human neurokinin-1 receptor antagonist.
Hale JJ, Mills SG, MacCoss M, Shah SK, Qi H, Mathre DJ, Cascieri MA, Sadowski S, Strader CD, MacIntyre DE, Metzger JM.
J Med Chem (1996) 39 : 1760 -1762
PubMed 8627597 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.18 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441225 CP-99994 1 5.40
CHEMBL52330 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441225 CP-99994 IC50 = 4000.0 nM 5.40
CHEMBL52330 IC50 = 11000.0 nM 4.96