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Assay Detail

CHEMBL3361464

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

Binding
Displacement of [125I]neurotensin from rat NTS2 receptor expressed in CHO-K1 cells by competitive binding assay
4
Total Activities
4
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-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.
Thomas JB, Giddings AM, Wiethe RW, Olepu S, Warner KR, Sarret P, Gendron L, Longpre JM, Zhang Y, Runyon SP, Gilmour BP.
J Med Chem (2014) 57 : 7472 -7477
PubMed 25157640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.08 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3040381 1 8.24
CHEMBL407196 NEUROTENSIN 1 7.55
CHEMBL3326831 1 6.70
CHEMBL3326832 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3040381 Ki = 5.8 nM 8.24
CHEMBL407196 NEUROTENSIN Ki = 28.0 nM 7.55
CHEMBL3326831 Ki = 202.0 nM 6.70
CHEMBL3326832 Ki = 1504.0 nM 5.82