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Assay Detail

CHEMBL1763145

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

Binding
Displacement [3H]SB-222200 from of human recombinant NK3 receptor expressed in CHO cells
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.
Hoveyda HR, Roy MO, Blanc S, Noël S, Salvino JM, Ator MA, Fraser G.
Bioorg Med Chem Lett (2011) 21 : 1991 -1996
PubMed 21376585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 6.32 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1760332 1 7.70
CHEMBL1760198 1 6.92
CHEMBL1760349 1 6.72
CHEMBL1760333 1 6.62
CHEMBL1760204 1 6.62
CHEMBL1760338 1 6.60
CHEMBL1760213 1 6.58
CHEMBL1760209 1 6.51
CHEMBL1760207 1 6.46
CHEMBL1760202 1 6.43
CHEMBL1760206 1 6.43
CHEMBL1760331 1 6.40
CHEMBL1760339 1 6.31
CHEMBL1760210 1 6.29
CHEMBL1760337 1 6.28
CHEMBL1760205 1 6.27
CHEMBL1760212 1 6.16
CHEMBL1760200 1 5.96
CHEMBL1760336 1 5.80
CHEMBL1306947 1 5.75
CHEMBL1760335 1 5.60
CHEMBL1760217 1 5.54
CHEMBL1760214 1 5.44
CHEMBL1760215 1 -
CHEMBL1760208 1 -
CHEMBL1760340 1 -
CHEMBL1760341 1 -
CHEMBL1760342 1 -
CHEMBL1760343 1 -
CHEMBL1760203 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1760332 Ki = 20.0 nM 7.70
CHEMBL1760198 Ki = 120.0 nM 6.92
CHEMBL1760349 Ki = 190.0 nM 6.72
CHEMBL1760333 Ki = 240.0 nM 6.62
CHEMBL1760204 Ki = 240.0 nM 6.62
CHEMBL1760338 Ki = 250.0 nM 6.60
CHEMBL1760213 Ki = 260.0 nM 6.58
CHEMBL1760209 Ki = 310.0 nM 6.51
CHEMBL1760207 Ki = 350.0 nM 6.46
CHEMBL1760202 Ki = 370.0 nM 6.43
CHEMBL1760206 Ki = 370.0 nM 6.43
CHEMBL1760331 Ki = 400.0 nM 6.40
CHEMBL1760339 Ki = 490.0 nM 6.31
CHEMBL1760210 Ki = 510.0 nM 6.29
CHEMBL1760337 Ki = 530.0 nM 6.28
CHEMBL1760205 Ki = 540.0 nM 6.27
CHEMBL1760212 Ki = 700.0 nM 6.16
CHEMBL1760200 Ki = 1100.0 nM 5.96
CHEMBL1760336 Ki = 1600.0 nM 5.80
CHEMBL1306947 Ki = 1800.0 nM 5.75
CHEMBL1760335 Ki = 2500.0 nM 5.60
CHEMBL1760217 Ki = 2900.0 nM 5.54
CHEMBL1760214 Ki = 3600.0 nM 5.44
CHEMBL1760216 Ki - -
CHEMBL1760334 Ki - -
CHEMBL1760350 Ki - -
CHEMBL1760218 Ki - -
CHEMBL1760199 Ki - -
CHEMBL1760348 Ki - -
CHEMBL1760347 Ki - -
CHEMBL1760211 Ki - -
CHEMBL1760346 Ki - -
CHEMBL1760345 Ki - -
CHEMBL1760219 Ki - -
CHEMBL1760215 Ki - -
CHEMBL1760197 Ki - -
CHEMBL1760201 Ki - -
CHEMBL1760344 Ki - -
CHEMBL1760203 Ki - -
CHEMBL1760343 Ki - -
CHEMBL1760342 Ki - -
CHEMBL1760341 Ki - -
CHEMBL1760340 Ki - -
CHEMBL1760208 Ki - -