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Assay Detail

CHEMBL863451

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

Binding
Displacement of [3H]citalopram from SERT
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.
Grundt P, Kopajtic TA, Katz JL, Newman AH.
Bioorg Med Chem Lett (2005) 15 : 5419 -5423
PubMed 16213721 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.41 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3085018 1 6.46
CHEMBL3085030 1 6.30
CHEMBL3085031 1 6.22
CHEMBL3085029 1 5.58
CHEMBL3085032 1 5.52
CHEMBL317757 DIFLUOROBENZTROPINE 1 5.49
CHEMBL3085028 1 5.41
CHEMBL3085027 1 5.38
CHEMBL3085024 1 5.38
CHEMBL3350391 1 5.06
CHEMBL3085023 1 4.96
CHEMBL3085025 1 4.87
CHEMBL3085033 1 4.76
CHEMBL3085019 1 4.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3085018 Ki = 347.0 nM 6.46
CHEMBL3085030 Ki = 502.0 nM 6.30
CHEMBL3085031 Ki = 608.0 nM 6.22
CHEMBL3085029 Ki = 2640.0 nM 5.58
CHEMBL3085032 Ki = 3010.0 nM 5.52
CHEMBL317757 DIFLUOROBENZTROPINE Ki = 3260.0 nM 5.49
CHEMBL3085028 Ki = 3920.0 nM 5.41
CHEMBL3085027 Ki = 4150.0 nM 5.38
CHEMBL3085024 Ki = 4180.0 nM 5.38
CHEMBL3350391 Ki = 8685.0 nM 5.06
CHEMBL3085023 Ki = 10900.0 nM 4.96
CHEMBL3085025 Ki = 13600.0 nM 4.87
CHEMBL3085033 Ki = 17200.0 nM 4.76
CHEMBL3085019 Ki = 48500.0 nM 4.31