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Assay Detail

CHEMBL992211

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

Binding
Binding affinity to NK3 receptor
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

New quinoline NK3 receptor antagonists with CNS activity.
Smith PW, Wyman PA, Lovell P, Goodacre C, Serafinowska HT, Vong A, Harrington F, Flynn S, Bradley DM, Porter R, Coggon S, Murkitt G, Searle K, Thomas DR, Watson JM, Martin W, Wu Z, Dawson LA.
Bioorg Med Chem Lett (2009) 19 : 837 -840
PubMed 19117759 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.28 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479463 1 9.00
CHEMBL519770 1 8.90
CHEMBL521416 1 8.90
CHEMBL480249 1 8.80
CHEMBL480818 1 8.70
CHEMBL479652 1 8.50
CHEMBL516441 1 8.40
CHEMBL517689 5-(3-METHYL-1-TRIAZENO)IMIDAZOLE-4-CARBOXAMIDE 1 8.30
CHEMBL517691 1 8.30
CHEMBL480248 1 8.20
CHEMBL519790 1 8.20
CHEMBL479450 1 8.10
CHEMBL10284 SB-222200 1 8.10
CHEMBL482006 1 8.00
CHEMBL480628 1 8.00
CHEMBL479449 1 7.80
CHEMBL520086 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479463 Ki = 1.0 nM 9.00
CHEMBL519770 Ki = 1.259 nM 8.90
CHEMBL521416 Ki = 1.259 nM 8.90
CHEMBL480249 Ki = 1.585 nM 8.80
CHEMBL480818 Ki = 1.995 nM 8.70
CHEMBL479652 Ki = 3.162 nM 8.50
CHEMBL516441 Ki = 3.981 nM 8.40
CHEMBL517689 5-(3-METHYL-1-TRIAZENO)IMIDAZOLE-4-CARBOXAMIDE Ki = 5.012 nM 8.30
CHEMBL517691 Ki = 5.012 nM 8.30
CHEMBL480248 Ki = 6.31 nM 8.20
CHEMBL519790 Ki = 6.31 nM 8.20
CHEMBL479450 Ki = 7.943 nM 8.10
CHEMBL10284 SB-222200 Ki = 7.943 nM 8.10
CHEMBL482006 Ki = 10.0 nM 8.00
CHEMBL480628 Ki = 10.0 nM 8.00
CHEMBL479449 Ki = 15.85 nM 7.80
CHEMBL520086 Ki = 251.19 nM 6.60