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Assay Detail

CHEMBL915898

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Binding
Displacement of [3H]WIN-35428 from DAT
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Sodium-dependent dopamine transporter (CHEMBL238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and monoamine transporter binding properties of 2,3-diaryltropanes.
Kotturi SV, Jiang S, Chang AC, Abraham P, Navarro HA, Kuhar MJ, Carroll FI.
J Med Chem (2005) 48 : 7437 -7444
PubMed 16279803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.51 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225235 1 9.05
CHEMBL224062 1 8.91
CHEMBL2096877 1 8.87
CHEMBL312037 2 8.77
CHEMBL224771 1 8.71
CHEMBL388850 1 7.90
CHEMBL387758 1 7.65
CHEMBL83729 1 7.64
CHEMBL388605 1 7.63
CHEMBL370805 COCAINE 4.0 1 7.05
CHEMBL2096878 1 6.62
CHEMBL426178 1 6.47
CHEMBL2096875 1 6.37
CHEMBL2096876 1 6.27
CHEMBL2096874 1 6.16
CHEMBL388825 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225235 IC50 = 0.9 nM 9.05
CHEMBL224062 IC50 = 1.23 nM 8.91
CHEMBL2096877 IC50 = 1.35 nM 8.87
CHEMBL312037 IC50 = 1.7 nM 8.77
CHEMBL224771 IC50 = 1.96 nM 8.71
CHEMBL388850 IC50 = 12.6 nM 7.90
CHEMBL387758 IC50 = 22.4 nM 7.65
CHEMBL83729 IC50 = 23.0 nM 7.64
CHEMBL388605 IC50 = 23.3 nM 7.63
CHEMBL312037 IC50 = 23.4 nM 7.63
CHEMBL370805 COCAINE IC50 = 89.1 nM 7.05
CHEMBL2096878 IC50 = 238.0 nM 6.62
CHEMBL426178 IC50 = 340.0 nM 6.47
CHEMBL2096875 IC50 = 430.0 nM 6.37
CHEMBL2096876 IC50 = 540.0 nM 6.27
CHEMBL2096874 IC50 = 690.0 nM 6.16
CHEMBL388825 IC50 = 980.0 nM 6.01