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Assay Detail

CHEMBL801199

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

Binding
Binding affinity of [3H]citalopram for serotonin transporter in monkey
11
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cercopithecidae
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of an unusually selective and novel cocaine analog: difluoropine. Synthesis and inhibition of binding at cocaine recognition sites.
Meltzer PC, Liang AY, Madras BK.
J Med Chem (1994) 37 : 2001 -2010
PubMed 8027983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.80 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300226 1 8.60
CHEMBL2079586 1 6.80
CHEMBL607430 2 5.84
CHEMBL607431 1 5.74
CHEMBL607377 4 5.70
CHEMBL310650 1 5.45
CHEMBL1201203 BENZTROPINE 4.0 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300226 IC50 = 2.53 nM 8.60
CHEMBL2079586 IC50 = 160.0 nM 6.80
CHEMBL607430 IC50 = 1460.0 nM 5.84
CHEMBL607431 IC50 = 1830.0 nM 5.74
CHEMBL607377 IC50 = 1980.0 nM 5.70
CHEMBL310650 IC50 = 3530.0 nM 5.45
CHEMBL607377 IC50 = 4087.0 nM 5.39
CHEMBL607377 IC50 = 4930.0 nM 5.31
CHEMBL607430 IC50 = 5500.0 nM 5.26
CHEMBL607377 IC50 = 9150.0 nM 5.04
CHEMBL1201203 BENZTROPINE IC50 = 24100.0 nM 4.62