Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5621453

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

Functional
Antagonist activity at human NK3R expressed in HEK293T cells assessed as reduction in NKB induced calcium signal incubated for 30 mins by FLIPR assay
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuromedin-K receptor (CHEMBL4429) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of piperazinotriazoles. Discovery of a potent and orally bioavailable neurokinin-3 receptor inhibitor.
Ye L, Yang Y, Li C, Zhang J, Wang W, Ma M, Xu H, Zhang W, Zou F, Hu Z, Wang H, Tian J.
Eur J Med Chem (2023) 257 : 115486 -115486
PubMed 37247507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 6.09 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5631018 — — 1 7.76
CHEMBL3422018 — — 1 7.53
CHEMBL5625091 — — 1 6.65
CHEMBL5625030 — — 1 6.56
CHEMBL5630439 — — 1 6.53
CHEMBL5630463 — — 1 6.51
CHEMBL5630592 — — 1 6.37
CHEMBL5630574 — — 1 6.37
CHEMBL5624800 — — 1 6.33
CHEMBL5630784 — — 1 6.31
CHEMBL5624666 — — 1 6.31
CHEMBL3608680 FEZOLINETANT 4.0 1 6.30
CHEMBL5624614 — — 1 6.23
CHEMBL5624825 — — 1 6.13
CHEMBL5630897 — — 1 6.05
CHEMBL5631195 — — 1 5.91
CHEMBL5624619 — — 1 5.89
CHEMBL5630243 — — 1 5.82
CHEMBL5624693 — — 1 5.82
CHEMBL5630966 — — 1 5.80
CHEMBL5631093 — — 1 5.78
CHEMBL5630303 — — 1 5.75
CHEMBL5624928 — — 1 5.51
CHEMBL5630470 — — 1 5.45
CHEMBL5630096 — — 1 5.42
CHEMBL5630142 — — 1 5.42
CHEMBL5624987 — — 1 5.34
CHEMBL5631189 — — 1 5.33
CHEMBL5631119 — — 1 5.29
CHEMBL5630542 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5631018 — IC50 = 17.26 nM 7.76
CHEMBL3422018 — IC50 = 29.51 nM 7.53
CHEMBL5625091 — IC50 = 224.51 nM 6.65
CHEMBL5625030 — IC50 = 276.32 nM 6.56
CHEMBL5630439 — IC50 = 296.92 nM 6.53
CHEMBL5630463 — IC50 = 307.35 nM 6.51
CHEMBL5630592 — IC50 = 430.6 nM 6.37
CHEMBL5630574 — IC50 = 430.16 nM 6.37
CHEMBL5624800 — IC50 = 462.6 nM 6.33
CHEMBL5630784 — IC50 = 489.12 nM 6.31
CHEMBL5624666 — IC50 = 487.42 nM 6.31
CHEMBL3608680 FEZOLINETANT IC50 = 500.83 nM 6.30
CHEMBL5624614 — IC50 = 594.91 nM 6.23
CHEMBL5624825 — IC50 = 741.42 nM 6.13
CHEMBL5630897 — IC50 = 881.94 nM 6.05
CHEMBL5631195 — IC50 = 1228.0 nM 5.91
CHEMBL5624619 — IC50 = 1277.36 nM 5.89
CHEMBL5630243 — IC50 = 1501.84 nM 5.82
CHEMBL5624693 — IC50 = 1523.56 nM 5.82
CHEMBL5630966 — IC50 = 1586.01 nM 5.80
CHEMBL5631093 — IC50 = 1646.61 nM 5.78
CHEMBL5630303 — IC50 = 1772.07 nM 5.75
CHEMBL5624928 — IC50 = 3087.02 nM 5.51
CHEMBL5630470 — IC50 = 3565.33 nM 5.45
CHEMBL5630096 — IC50 = 3782.84 nM 5.42
CHEMBL5630142 — IC50 = 3815.38 nM 5.42
CHEMBL5624987 — IC50 = 4560.84 nM 5.34
CHEMBL5631189 — IC50 = 4625.06 nM 5.33
CHEMBL5631119 — IC50 = 5144.08 nM 5.29
CHEMBL5624894 — IC50 > 10000.0 nM -
CHEMBL5630830 — IC50 > 10000.0 nM -
CHEMBL5629992 — IC50 > 10000.0 nM -
CHEMBL5624892 — IC50 > 10000.0 nM -
CHEMBL5624882 — IC50 > 10000.0 nM -
CHEMBL5630156 — IC50 > 10000.0 nM -
CHEMBL5630935 — IC50 > 10000.0 nM -
CHEMBL5630076 — IC50 > 10000.0 nM -
CHEMBL5631127 — IC50 > 10000.0 nM -
CHEMBL5630528 — IC50 > 10000.0 nM -
CHEMBL5624770 — IC50 > 10000.0 nM -
CHEMBL5630079 — IC50 > 10000.0 nM -
CHEMBL5624456 — IC50 > 10000.0 nM -
CHEMBL5630542 — IC50 > 10000.0 nM -