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Assay Detail

CHEMBL809439

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

Binding
In vitro binding affinity for serotonin reuptake sites in rat frontal cortex membranes by [3H]paroxetine displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition.
van Hes R, Smid P, Stroomer CN, Tipker K, Tulp MT, van der Heyden JA, McCreary AC, Hesselink MB, Kruse CG.
Bioorg Med Chem Lett (2003) 13 : 405 -408
PubMed 12565939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.70 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL335844 1 9.40
CHEMBL131495 1 9.22
CHEMBL338270 1 9.10
CHEMBL339098 1 9.10
CHEMBL335259 1 9.00
CHEMBL129852 1 9.00
CHEMBL422618 1 8.89
CHEMBL336771 1 8.89
CHEMBL421902 1 8.70
CHEMBL423706 1 8.70
CHEMBL130261 1 8.70
CHEMBL414433 1 8.60
CHEMBL133524 1 8.60
CHEMBL276520 INDALPINE 4.0 1 8.60
CHEMBL340220 1 8.52
CHEMBL27811 1 8.22
CHEMBL129979 1 7.80
CHEMBL334956 1 7.60
CHEMBL54 HALOPERIDOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL335844 Ki = 0.4 nM 9.40
CHEMBL131495 Ki = 0.6 nM 9.22
CHEMBL338270 Ki = 0.8 nM 9.10
CHEMBL339098 Ki = 0.8 nM 9.10
CHEMBL335259 Ki = 1.0 nM 9.00
CHEMBL129852 Ki = 1.0 nM 9.00
CHEMBL422618 Ki = 1.3 nM 8.89
CHEMBL336771 Ki = 1.3 nM 8.89
CHEMBL421902 Ki = 2.0 nM 8.70
CHEMBL423706 Ki = 2.0 nM 8.70
CHEMBL130261 Ki = 2.0 nM 8.70
CHEMBL414433 Ki = 2.5 nM 8.60
CHEMBL133524 Ki = 2.5 nM 8.60
CHEMBL276520 INDALPINE Ki = 2.5 nM 8.60
CHEMBL340220 Ki = 3.0 nM 8.52
CHEMBL27811 Ki = 6.0 nM 8.22
CHEMBL129979 Ki = 16.0 nM 7.80
CHEMBL334956 Ki = 25.0 nM 7.60
CHEMBL54 HALOPERIDOL Ki > 1000.0 nM -