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Assay Detail

CHEMBL954043

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

Binding
Inhibition of [3H]5HT uptake at SERT in rat cortical synaptosomes
22
Total Activities
22
Compounds Tested
1
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

Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
Ward SE, Eddershaw PJ, Scott CM, Gordon LJ, Lovell PJ, Moore SH, Smith PW, Starr KR, Thewlis KM, Watson JM.
J Med Chem (2008) 51 : 2887 -2890
PubMed 18433113 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.28 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183460 1 8.00
CHEMBL498356 1 7.10
CHEMBL495895 1 6.70
CHEMBL525362 1 6.60
CHEMBL425190 1 6.50
CHEMBL494991 1 6.40
CHEMBL496098 1 6.40
CHEMBL495213 1 6.40
CHEMBL525712 1 6.30
CHEMBL498355 1 6.30
CHEMBL494992 1 6.20
CHEMBL495217 1 6.20
CHEMBL522708 1 6.10
CHEMBL494631 1 6.10
CHEMBL497127 1 6.10
CHEMBL498354 1 6.10
CHEMBL495046 1 6.00
CHEMBL497963 1 6.00
CHEMBL506942 1 6.00
CHEMBL494806 1 5.90
CHEMBL495160 1 5.80
CHEMBL495161 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183460 Ki = 10.0 nM 8.00
CHEMBL498356 Ki = 79.43 nM 7.10
CHEMBL495895 Ki = 199.53 nM 6.70
CHEMBL525362 Ki = 251.19 nM 6.60
CHEMBL425190 Ki = 316.23 nM 6.50
CHEMBL494991 Ki = 398.11 nM 6.40
CHEMBL496098 Ki = 398.11 nM 6.40
CHEMBL495213 Ki = 398.11 nM 6.40
CHEMBL525712 Ki = 501.19 nM 6.30
CHEMBL498355 Ki = 501.19 nM 6.30
CHEMBL494992 Ki = 630.96 nM 6.20
CHEMBL495217 Ki = 630.96 nM 6.20
CHEMBL522708 Ki = 794.33 nM 6.10
CHEMBL494631 Ki = 794.33 nM 6.10
CHEMBL497127 Ki = 794.33 nM 6.10
CHEMBL498354 Ki = 794.33 nM 6.10
CHEMBL495046 Ki = 1000.0 nM 6.00
CHEMBL497963 Ki = 1000.0 nM 6.00
CHEMBL506942 Ki = 1000.0 nM 6.00
CHEMBL494806 Ki = 1258.93 nM 5.90
CHEMBL495160 Ki = 1584.89 nM 5.80
CHEMBL495161 Ki = 10000.0 nM 5.00