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Assay Detail

CHEMBL3373063

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

Functional
Agonist activity at rat neurotensin receptor type 2 expressed in CHOK1 cells assessed as increase in calcium release by FLIPR assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neurotensin receptor type 2 (CHEMBL5106)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
Thomas JB, Giddings AM, Olepu S, Wiethe RW, Harris DL, Narayanan S, Warner KR, Sarret P, Longpre JM, Runyon SP, Gilmour BP.
Bioorg Med Chem Lett (2015) 25 : 292 -296
PubMed 25499438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.48 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356854 1 7.85
CHEMBL3040381 1 7.75
CHEMBL3356853 1 6.84
CHEMBL407196 NEUROTENSIN 1 -
CHEMBL3356855 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356854 EC50 = 14.0 nM 7.85
CHEMBL3040381 EC50 = 18.0 nM 7.75
CHEMBL3356853 EC50 = 145.0 nM 6.84
CHEMBL407196 NEUROTENSIN EC50 > 100.0 nM -
CHEMBL3356855 EC50 > 10.0 nM -