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Assay Detail

CHEMBL3407205

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

Binding
Displacement of [I125]neurotensin from rat NTS1 overexpressed in CHO-k1 cells by competitive binding Assay
10
Total Activities
10
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 1 (CHEMBL3027)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The amide linker in nonpeptide neurotensin receptor ligands plays a key role in calcium signaling at the neurotensin receptor type 2.
Thomas JB, Giddings AM, Olepu S, Wiethe RW, Warner KR, Sarret P, Longpre JM, Runyon SP, Gilmour BP.
Bioorg Med Chem Lett (2015) 25 : 2060 -2064
PubMed 25881832 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.66 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3290096 1 6.75
CHEMBL3290101 1 5.92
CHEMBL3290105 1 5.49
CHEMBL3403505 1 5.14
CHEMBL3403506 1 4.99
CHEMBL461604 1 -
CHEMBL3403504 1 -
CHEMBL3403507 1 -
CHEMBL3290106 1 -
CHEMBL3403508 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3290096 Ki = 177.0 nM 6.75
CHEMBL3290101 Ki = 1210.0 nM 5.92
CHEMBL3290105 Ki = 3210.0 nM 5.49
CHEMBL3403505 Ki = 7181.0 nM 5.14
CHEMBL3403506 Ki = 10162.0 nM 4.99
CHEMBL461604 Ki - -
CHEMBL3403504 Ki > 10000.0 nM -
CHEMBL3403507 Ki > 25000.0 nM -
CHEMBL3290106 Ki > 25000.0 nM -
CHEMBL3403508 Ki > 25000.0 nM -