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Assay Detail

CHEMBL804974

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

Binding
Displacement of [3H]-citalopram from serotonin transporter of rat brain membrane
13
Total Activities
13
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 Expert

Target

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

Publication

The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor.
Grundt P, Kopajtic TA, Katz JL, Newman AH.
Bioorg Med Chem Lett (2004) 14 : 3295 -3298
PubMed 15149693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.20 6.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370805 COCAINE 4.0 1 6.53
CHEMBL317757 DIFLUOROBENZTROPINE 1 5.49
CHEMBL2112513 1 5.43
CHEMBL2112516 1 5.35
CHEMBL2112511 1 5.23
CHEMBL2112514 1 5.10
CHEMBL2112512 1 5.10
CHEMBL113144 1 5.08
CHEMBL113195 1 4.93
CHEMBL2112515 1 4.86
CHEMBL2112509 1 4.85
CHEMBL2112510 1 4.83
CHEMBL2112508 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370805 COCAINE Ki = 293.0 nM 6.53
CHEMBL317757 DIFLUOROBENZTROPINE Ki = 3260.0 nM 5.49
CHEMBL2112513 Ki = 3730.0 nM 5.43
CHEMBL2112516 Ki = 4440.0 nM 5.35
CHEMBL2112511 Ki = 5850.0 nM 5.23
CHEMBL2112514 Ki = 7960.0 nM 5.10
CHEMBL2112512 Ki = 7960.0 nM 5.10
CHEMBL113144 Ki = 8290.0 nM 5.08
CHEMBL113195 Ki = 11700.0 nM 4.93
CHEMBL2112515 Ki = 13800.0 nM 4.86
CHEMBL2112509 Ki = 14000.0 nM 4.85
CHEMBL2112510 Ki = 14800.0 nM 4.83
CHEMBL2112508 Ki = 16500.0 nM 4.78