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Assay Detail

CHEMBL747997

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

Binding
Displacement of [3H]-nisoxatine from norepinephrine transporter of rat brain membrane
14
Total Activities
14
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

Norepinephrine transporter (CHEMBL304)
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 14 5.45 6.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317757 DIFLUOROBENZTROPINE 1 6.07
CHEMBL112825 1 5.89
CHEMBL2112513 1 5.86
CHEMBL113144 1 5.86
CHEMBL2112516 1 5.50
CHEMBL370805 COCAINE 4.0 1 5.48
CHEMBL2112509 1 5.43
CHEMBL2112514 1 5.25
CHEMBL2112511 1 5.21
CHEMBL113195 1 5.19
CHEMBL2112512 1 5.18
CHEMBL2112515 1 5.16
CHEMBL2112508 1 5.16
CHEMBL2112510 1 4.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317757 DIFLUOROBENZTROPINE Ki = 844.0 nM 6.07
CHEMBL112825 Ki = 1300.0 nM 5.89
CHEMBL2112513 Ki = 1370.0 nM 5.86
CHEMBL113144 Ki = 1380.0 nM 5.86
CHEMBL2112516 Ki = 3170.0 nM 5.50
CHEMBL370805 COCAINE Ki = 3302.0 nM 5.48
CHEMBL2112509 Ki = 3720.0 nM 5.43
CHEMBL2112514 Ki = 5690.0 nM 5.25
CHEMBL2112511 Ki = 6206.0 nM 5.21
CHEMBL113195 Ki = 6390.0 nM 5.19
CHEMBL2112512 Ki = 6610.0 nM 5.18
CHEMBL2112515 Ki = 6880.0 nM 5.16
CHEMBL2112508 Ki = 6910.0 nM 5.16
CHEMBL2112510 Ki = 10200.0 nM 4.99