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Assay Detail

CHEMBL745033

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

Binding
Displacement of [3H]- NKA from human NK-2 receptor expressed in MEL cells
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type MEL
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Substance-K receptor (CHEMBL2327)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Alkylpiperidines related to SR-48968: potent antagonists of the neurokinin-2 (NK2) receptor.
Jacobs RT, Shenvi AB, Mauger RC, Ulatowski TG, Aharony D, Buckner CK.
Bioorg Med Chem Lett (1998) 8 : 1935 -1940
PubMed 9873462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.15 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56835 2 9.22
CHEMBL2115073 1 9.08
CHEMBL443264 1 8.89
CHEMBL2111522 1 8.68
CHEMBL2115072 1 8.57
CHEMBL56481 1 8.46
CHEMBL56788 1 8.43
CHEMBL56143 1 8.33
CHEMBL58638 1 8.19
CHEMBL301437 1 8.11
CHEMBL417940 1 8.04
CHEMBL59542 1 8.00
CHEMBL56739 1 7.88
CHEMBL56274 1 7.47
CHEMBL57589 1 7.40
CHEMBL292415 1 7.33
CHEMBL58331 1 7.18
CHEMBL57224 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56835 Ki = 0.6 nM 9.22
CHEMBL2115073 Ki = 0.84 nM 9.08
CHEMBL443264 Ki = 1.3 nM 8.89
CHEMBL56835 Ki = 1.75 nM 8.76
CHEMBL2111522 Ki = 2.1 nM 8.68
CHEMBL2115072 Ki = 2.7 nM 8.57
CHEMBL56481 Ki = 3.5 nM 8.46
CHEMBL56788 Ki = 3.7 nM 8.43
CHEMBL56143 Ki = 4.7 nM 8.33
CHEMBL58638 Ki = 6.5 nM 8.19
CHEMBL301437 Ki = 7.7 nM 8.11
CHEMBL417940 Ki = 9.2 nM 8.04
CHEMBL59542 Ki = 9.9 nM 8.00
CHEMBL56739 Ki = 13.1 nM 7.88
CHEMBL56274 Ki = 33.5 nM 7.47
CHEMBL57589 Ki = 40.0 nM 7.40
CHEMBL292415 Ki = 47.0 nM 7.33
CHEMBL58331 Ki = 66.0 nM 7.18
CHEMBL57224 Ki = 142.0 nM 6.85