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Assay Detail

CHEMBL3373067

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

Binding
Displacement of [125L]NT from rat neurotensin receptor type 2 expressed in CHOK1 cells by radioligand binding assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 5 7.05 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3040381 1 8.15
CHEMBL407196 NEUROTENSIN 1 7.68
CHEMBL3356854 1 7.06
CHEMBL3356855 1 6.32
CHEMBL3356853 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3040381 Ki = 7.0 nM 8.15
CHEMBL407196 NEUROTENSIN Ki = 21.0 nM 7.68
CHEMBL3356854 Ki = 88.0 nM 7.06
CHEMBL3356855 Ki = 474.0 nM 6.32
CHEMBL3356853 Ki = 959.0 nM 6.02