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Assay Detail

CHEMBL963296

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Functional
Agonist activity at NTR1 expressed in CHOK1 cells by calcium mobilization assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Neurotensin receptor type 1 (CHEMBL4123)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.
Thomas JB, Navarro H, Warner KR, Gilmour B.
Bioorg Med Chem Lett (2009) 19 : 1438 -1441
PubMed 19195889 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.81 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407196 NEUROTENSIN 1 9.64
CHEMBL508044 1 7.17
CHEMBL463811 1 6.75
CHEMBL294989 1 6.67
CHEMBL462830 1 6.66
CHEMBL463227 1 6.01
CHEMBL518675 1 5.92
CHEMBL464011 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407196 NEUROTENSIN EC50 = 0.23 nM 9.64
CHEMBL508044 EC50 = 67.0 nM 7.17
CHEMBL463811 EC50 = 178.0 nM 6.75
CHEMBL294989 EC50 = 216.0 nM 6.67
CHEMBL462830 EC50 = 220.0 nM 6.66
CHEMBL463227 EC50 = 986.0 nM 6.01
CHEMBL518675 EC50 = 1214.0 nM 5.92
CHEMBL464011 EC50 = 2043.0 nM 5.69