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Assay Detail

CHEMBL3377149

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

Binding
Induction of DAT-mediated dopamine release in rat brain synaptosomes by [3H]DA release assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Synaptosomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Alpha-ethyltryptamines as dual dopamine-serotonin releasers.
Blough BE, Landavazo A, Partilla JS, Decker AM, Page KM, Baumann MH, Rothman RB.
Bioorg Med Chem Lett (2014) 24 : 4754 -4758
PubMed 25193229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 6.61 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL471839 1 7.90
CHEMBL96816 1 7.43
CHEMBL1906905 1 7.26
CHEMBL3330646 1 7.24
CHEMBL30713 1 7.11
CHEMBL275628 1 7.08
CHEMBL382635 1 6.97
CHEMBL381160 1 6.97
CHEMBL337825 1 6.95
CHEMBL3330648 1 6.82
CHEMBL6640 TRYPTAMINE 1 6.79
CHEMBL1619758 ETRYPTAMINE 2.0 1 6.63
CHEMBL348588 1 6.49
CHEMBL3330642 1 6.45
CHEMBL1288717 1 6.32
CHEMBL1288716 1 6.32
CHEMBL3330645 1 6.18
CHEMBL3330643 1 5.88
CHEMBL3330644 1 5.67
CHEMBL204839 1 5.47
CHEMBL8165 5-METHOXYTRYPTAMINE 1 4.96
CHEMBL331241 1 -
CHEMBL343529 1 -
CHEMBL3330641 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL471839 EC50 = 12.6 nM 7.90
CHEMBL96816 EC50 = 37.0 nM 7.43
CHEMBL1906905 EC50 = 54.3 nM 7.26
CHEMBL3330646 EC50 = 57.6 nM 7.24
CHEMBL30713 EC50 = 78.6 nM 7.11
CHEMBL275628 EC50 = 82.3 nM 7.08
CHEMBL382635 EC50 = 106.0 nM 6.97
CHEMBL381160 EC50 = 106.0 nM 6.97
CHEMBL337825 EC50 = 113.0 nM 6.95
CHEMBL3330648 EC50 = 150.0 nM 6.82
CHEMBL6640 TRYPTAMINE EC50 = 164.0 nM 6.79
CHEMBL1619758 ETRYPTAMINE EC50 = 232.0 nM 6.63
CHEMBL348588 EC50 = 321.0 nM 6.49
CHEMBL3330642 EC50 = 353.0 nM 6.45
CHEMBL1288717 EC50 = 478.0 nM 6.32
CHEMBL1288716 EC50 = 476.0 nM 6.32
CHEMBL3330645 EC50 = 654.0 nM 6.18
CHEMBL3330643 EC50 = 1330.0 nM 5.88
CHEMBL3330644 EC50 = 2118.0 nM 5.67
CHEMBL204839 EC50 = 3380.0 nM 5.47
CHEMBL8165 5-METHOXYTRYPTAMINE EC50 = 11031.0 nM 4.96
CHEMBL331241 EC50 > 10000.0 nM -
CHEMBL343529 EC50 > 10000.0 nM -
CHEMBL3330641 EC50 > 10000.0 nM -