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Assay Detail

CHEMBL872827

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

Functional
Inhibition of dopamine reuptake ([3H]DA uptake) in rat cytosol
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Structure-activity relationship studies of 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives and their N-analogues: evaluation of O-and N-analogues and their binding to monoamine transporters.
Dutta AK, Fei XS, Beardsley PM, Newman JL, Reith ME.
J Med Chem (2001) 44 : 937 -948
PubMed 11300876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.98 8.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20648 1 8.61
CHEMBL35239 1 8.34
CHEMBL281594 VANOXERINE 3.0 1 8.18
CHEMBL353643 1 8.01
CHEMBL369406 1 7.97
CHEMBL110530 1 7.92
CHEMBL424005 1 7.78
CHEMBL159128 1 7.69
CHEMBL39262 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20648 IC50 = 2.48 nM 8.61
CHEMBL35239 IC50 = 4.58 nM 8.34
CHEMBL281594 VANOXERINE IC50 = 6.63 nM 8.18
CHEMBL353643 IC50 = 9.73 nM 8.01
CHEMBL369406 IC50 = 10.7 nM 7.97
CHEMBL110530 IC50 = 12.0 nM 7.92
CHEMBL424005 IC50 = 16.6 nM 7.78
CHEMBL159128 IC50 = 20.6 nM 7.69
CHEMBL39262 IC50 = 49.6 nM 7.30