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Assay Detail

CHEMBL990614

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

Binding
Inhibition of [3H]5HT reuptake at SERT in rat cortical synaptosomes
16
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel 5-HT(1A/1B/1D) receptors antagonists with potent 5-HT reuptake inhibitory activity.
Serafinowska HT, Blaney FE, Lovell PJ, Merlo GG, Scott CM, Smith PW, Starr KR, Watson JM.
Bioorg Med Chem Lett (2008) 18 : 5581 -5585
PubMed 18829312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.23 8.40
Activity 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490417 1 8.40
CHEMBL483365 1 8.20
CHEMBL183460 1 8.10
CHEMBL485395 1 7.60
CHEMBL484743 1 7.50
CHEMBL484387 1 7.20
CHEMBL485427 1 7.00
CHEMBL484742 1 6.70
CHEMBL484386 1 6.60
CHEMBL484205 1 6.10
CHEMBL485630 1 6.10
CHEMBL484216 2 -
CHEMBL519010 1 -
CHEMBL519019 1 -
CHEMBL519037 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490417 Ki = 3.981 nM 8.40
CHEMBL483365 Ki = 6.31 nM 8.20
CHEMBL183460 Ki = 7.943 nM 8.10
CHEMBL485395 Ki = 25.12 nM 7.60
CHEMBL484743 Ki = 31.62 nM 7.50
CHEMBL484387 Ki = 63.1 nM 7.20
CHEMBL485427 Ki = 100.0 nM 7.00
CHEMBL484742 Ki = 199.53 nM 6.70
CHEMBL484386 Ki = 251.19 nM 6.60
CHEMBL484205 Ki = 794.33 nM 6.10
CHEMBL485630 Ki = 794.33 nM 6.10
CHEMBL484216 Activity - -
CHEMBL484216 Activity - -
CHEMBL519010 Activity - -
CHEMBL519019 Activity - -
CHEMBL519037 Activity - -