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Assay Detail

CHEMBL1286482

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Functional
Agonist activity at rat DAT expressed in CHO cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery and synthesis of novel luteolin derivatives as DAT agonists.
Zhang J, Liu X, Lei X, Wang L, Guo L, Zhao G, Lin G.
Bioorg Med Chem (2010) 18 : 7842 -7848
PubMed 20971650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 26 5.45 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1277422 1 7.34
CHEMBL1277423 1 6.06
CHEMBL1278225 1 5.86
CHEMBL151 LUTEOLIN 2.0 1 5.84
CHEMBL1278140 1 5.77
CHEMBL1278139 1 5.77
CHEMBL1277333 1 5.74
CHEMBL1277702 1 5.66
CHEMBL1277795 1 5.62
CHEMBL1278046 1 5.59
CHEMBL1277515 1 5.57
CHEMBL1277703 1 5.51
CHEMBL1278226 1 5.47
CHEMBL1277878 1 5.46
CHEMBL1277701 1 5.36
CHEMBL1277879 1 5.34
CHEMBL1277796 1 5.32
CHEMBL1277242 1 5.27
CHEMBL1277794 1 5.26
CHEMBL1277610 1 5.16
CHEMBL1277516 1 5.07
CHEMBL1277609 1 4.95
CHEMBL1278227 1 4.89
CHEMBL1277960 1 4.78
CHEMBL1277332 1 4.51
CHEMBL1277961 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1277422 EC50 = 46.0 nM 7.34
CHEMBL1277423 EC50 = 869.0 nM 6.06
CHEMBL1278225 EC50 = 1375.0 nM 5.86
CHEMBL151 LUTEOLIN EC50 = 1450.0 nM 5.84
CHEMBL1278140 EC50 = 1694.0 nM 5.77
CHEMBL1278139 EC50 = 1696.0 nM 5.77
CHEMBL1277333 EC50 = 1820.0 nM 5.74
CHEMBL1277702 EC50 = 2213.0 nM 5.66
CHEMBL1277795 EC50 = 2401.92 nM 5.62
CHEMBL1278046 EC50 = 2594.0 nM 5.59
CHEMBL1277515 EC50 = 2706.0 nM 5.57
CHEMBL1277703 EC50 = 3072.0 nM 5.51
CHEMBL1278226 EC50 = 3417.0 nM 5.47
CHEMBL1277878 EC50 = 3428.0 nM 5.46
CHEMBL1277701 EC50 = 4345.0 nM 5.36
CHEMBL1277879 EC50 = 4575.0 nM 5.34
CHEMBL1277796 EC50 = 4798.0 nM 5.32
CHEMBL1277242 EC50 = 5368.0 nM 5.27
CHEMBL1277794 EC50 = 5430.0 nM 5.26
CHEMBL1277610 EC50 = 6920.0 nM 5.16
CHEMBL1277516 EC50 = 8557.0 nM 5.07
CHEMBL1277609 EC50 = 11174.0 nM 4.95
CHEMBL1278227 EC50 = 12856.0 nM 4.89
CHEMBL1277960 EC50 = 16521.0 nM 4.78
CHEMBL1277332 EC50 = 30978.0 nM 4.51
CHEMBL1277961 EC50 = 33002.0 nM 4.48