Assay Detail

CHEMBL814181

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Binding

compounds were evaluated for inhibitory activity against human Tachykinin receptor 1

ChEMBL ↗

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Target

Substance-P receptor (CHEMBL249) ↗

Open DB target context

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Substance-P receptor (CHEMBL249) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Substance-P receptor

CHEMBL249

Anchored from Assay target.

Protein identity Substance-P receptor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

Substance-P receptor (CHEMBL249) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Phosphorylated morpholine acetal human neurokinin-1 receptor antagonists as water-soluble prodrugs.

Hale JJ, Mills SG, MacCoss M, Dorn CP, Finke PE, Budhu RJ, Reamer RA, Huskey SE, Luffer-Atlas D, Dean BJ, McGowan EM, Feeney WP, Chiu SH, Cascieri MA, Chicchi GG, Kurtz MM, Sadowski S, Ber E, Tattersall FD, Rupniak NM, Williams AR, Rycroft W, Hargreaves R, Metzger JM, MacIntyre DE.
J Med Chem (2000) 43 : 1234 -1241
PubMed 10737756 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	10.05	10.05

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1471	APREPITANT	4.0	1	10.05

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1471	APREPITANT	IC50	=	0.09	nM	10.05