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Assay Detail

CHEMBL3610107

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Binding
Binding affinity to rat NK3R
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuromedin-K receptor (CHEMBL3154)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).
Hoveyda HR, Fraser GL, Dutheuil G, El Bousmaqui M, Korac J, Lenoir F, Lapin A, Noël S.
ACS Med Chem Lett (2015) 6 : 736 -740
PubMed 26191358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.72 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3422018 1 7.66
CHEMBL3422010 1 7.12
CHEMBL3608688 1 7.07
CHEMBL3608680 FEZOLINETANT 4.0 1 6.66
CHEMBL3608741 1 6.61
CHEMBL3608740 1 6.24
CHEMBL3608684 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3422018 Ki = 22.0 nM 7.66
CHEMBL3422010 Ki = 76.0 nM 7.12
CHEMBL3608688 Ki = 85.0 nM 7.07
CHEMBL3608680 FEZOLINETANT Ki = 219.0 nM 6.66
CHEMBL3608741 Ki = 244.0 nM 6.61
CHEMBL3608740 Ki = 573.0 nM 6.24
CHEMBL3608684 Ki = 2033.0 nM 5.69