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Assay Detail

CHEMBL3424997

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

Binding
Displacement of [3H]-SB222200 from recombinant human NK3R expressed in CHO cell membranes after 90 mins by scintillation counting analysis
41
Total Activities
39
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 and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).
Hoveyda HR, Fraser GL, Roy MO, Dutheuil G, Batt F, El Bousmaqui M, Korac J, Lenoir F, Lapin A, Noël S, Blanc S.
J Med Chem (2015) 58 : 3060 -3082
PubMed 25738882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 6.83 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL346178 OSANETANT 2.0 1 8.80
CHEMBL3422009 1 8.70
CHEMBL3422014 1 8.60
CHEMBL3422018 1 8.50
CHEMBL3422015 1 8.50
CHEMBL3422016 1 8.20
CHEMBL10188 TALNETANT 2.0 1 8.10
CHEMBL3422007 1 8.00
CHEMBL3422008 1 7.90
CHEMBL3422010 1 7.90
CHEMBL3422006 1 7.60
CHEMBL3422017 1 7.60
CHEMBL3421999 1 7.20
CHEMBL3421982 2 7.12
CHEMBL3422012 1 7.10
CHEMBL3422013 1 7.10
CHEMBL3422005 1 7.00
CHEMBL3422011 1 6.50
CHEMBL3422004 1 6.40
CHEMBL3421994 1 6.30
CHEMBL3422000 1 6.30
CHEMBL3421998 1 6.10
CHEMBL3421989 1 5.90
CHEMBL3422001 1 5.80
CHEMBL3421996 1 5.80
CHEMBL3421990 1 5.70
CHEMBL3421983 2 5.35
CHEMBL3421985 1 5.30
CHEMBL3421991 1 5.30
CHEMBL3422002 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL346178 OSANETANT Ki = 1.585 nM 8.80
CHEMBL3422009 Ki = 1.995 nM 8.70
CHEMBL3422014 Ki = 2.512 nM 8.60
CHEMBL3422018 Ki = 3.162 nM 8.50
CHEMBL3422015 Ki = 3.162 nM 8.50
CHEMBL3422016 Ki = 6.31 nM 8.20
CHEMBL10188 TALNETANT Ki = 7.943 nM 8.10
CHEMBL3422007 Ki = 10.0 nM 8.00
CHEMBL3422008 Ki = 12.59 nM 7.90
CHEMBL3422010 Ki = 12.59 nM 7.90
CHEMBL3422017 Ki = 25.12 nM 7.60
CHEMBL3422006 Ki = 25.12 nM 7.60
CHEMBL3421999 Ki = 63.1 nM 7.20
CHEMBL3421982 Ki = 76.0 nM 7.12
CHEMBL3422013 Ki = 79.43 nM 7.10
CHEMBL3422012 Ki = 79.43 nM 7.10
CHEMBL3421982 Ki = 79.43 nM 7.10
CHEMBL3422005 Ki = 100.0 nM 7.00
CHEMBL3422011 Ki = 316.23 nM 6.50
CHEMBL3422004 Ki = 398.11 nM 6.40
CHEMBL3421994 Ki = 501.19 nM 6.30
CHEMBL3422000 Ki = 501.19 nM 6.30
CHEMBL3421998 Ki = 794.33 nM 6.10
CHEMBL3421989 Ki = 1258.93 nM 5.90
CHEMBL3422001 Ki = 1584.89 nM 5.80
CHEMBL3421996 Ki = 1584.89 nM 5.80
CHEMBL3421990 Ki = 1995.26 nM 5.70
CHEMBL3421983 Ki = 4500.0 nM 5.35
CHEMBL3421983 Ki = 5011.87 nM 5.30
CHEMBL3421985 Ki = 5011.87 nM 5.30
CHEMBL3421991 Ki = 5011.87 nM 5.30
CHEMBL3422002 Ki = 6309.57 nM 5.20
CHEMBL3421997 Ki = 7943.28 nM 5.10
CHEMBL3421995 Ki = 15848.93 nM 4.80
CHEMBL3422003 Ki > 31622.78 nM -
CHEMBL3421984 Ki > 31622.78 nM -
CHEMBL3421986 Ki > 31622.78 nM -
CHEMBL3421987 Ki > 31622.78 nM -
CHEMBL3421988 Ki > 31622.78 nM -
CHEMBL3421992 Ki > 31622.78 nM -
CHEMBL3421993 Ki > 31622.78 nM -