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Assay Detail

CHEMBL992219

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

Functional
Binding affinity to NK3 receptor in gerbil cortex at 10 mg/kg, po
3
Total Activities
3
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Functional
Organism Gerbillinae
Confidence 1 — Organism
Curated By Autocuration

Target

Gerbillinae (CHEMBL612671)
Type ORGANISM
Organism Gerbillinae

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 3 8.43 8.90

Assay Parameters

Parameter Type Value Units Text
DOSE DOSE 10.0 mg.kg-1
ROUTE ROUTE - Oral

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479463 1 8.90
CHEMBL346178 OSANETANT 2.0 1 8.70
CHEMBL10188 TALNETANT 2.0 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479463 Ki = 1.259 nM 8.90
CHEMBL346178 OSANETANT Ki = 1.995 nM 8.70
CHEMBL10188 TALNETANT Ki = 19.95 nM 7.70