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Assay Detail

CHEMBL911127

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

Binding
Inhibition of [3H]5-HT uptake into human SERT expressing HEK293 cells
ChEMBL ↗
54
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL228) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Slow-onset, long-duration, alkyl analogues of methylphenidate with enhanced selectivity for the dopamine transporter.
Froimowitz M, Gu Y, Dakin LA, Nagafuji PM, Kelley CJ, Parrish D, Deschamps JR, Janowsky A.
J Med Chem (2007) 50 : 219 -232
PubMed 17228864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 5.79 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219649 — — 2 6.75
CHEMBL219281 — — 2 6.68
CHEMBL370805 COCAINE 4.0 1 6.60
CHEMBL218999 — — 2 6.54
CHEMBL220247 — — 2 6.31
CHEMBL220195 — — 2 6.27
CHEMBL374634 — — 2 6.26
CHEMBL219335 — — 2 6.06
CHEMBL219707 — — 2 6.00
CHEMBL373773 — — 2 5.96
CHEMBL441864 — — 2 5.92
CHEMBL218894 — — 2 5.92
CHEMBL218847 — — 2 5.89
CHEMBL387117 — — 2 5.85
CHEMBL219703 — — 2 5.82
CHEMBL218193 — — 2 5.77
CHEMBL374769 — — 2 5.75
CHEMBL219224 — — 2 5.72
CHEMBL219653 — — 2 5.68
CHEMBL376852 — — 2 5.62
CHEMBL217975 — — 2 5.58
CHEMBL218848 — — 1 5.48
CHEMBL218849 — — 2 5.48
CHEMBL375118 — — 2 5.38
CHEMBL796 METHYLPHENIDATE 4.0 1 5.29
CHEMBL373710 — — 2 5.14
CHEMBL219540 — — 1 -
CHEMBL219334 — — 2 -
CHEMBL219116 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219649 — IC50 = 180.0 nM 6.75
CHEMBL219281 — IC50 = 210.0 nM 6.68
CHEMBL370805 COCAINE IC50 = 250.0 nM 6.60
CHEMBL218999 — IC50 = 290.0 nM 6.54
CHEMBL220247 — IC50 = 490.0 nM 6.31
CHEMBL220247 — IC50 = 540.0 nM 6.27
CHEMBL220195 — IC50 = 540.0 nM 6.27
CHEMBL374634 — IC50 = 550.0 nM 6.26
CHEMBL219649 — IC50 = 560.0 nM 6.25
CHEMBL219281 — IC50 = 650.0 nM 6.19
CHEMBL219335 — IC50 = 870.0 nM 6.06
CHEMBL219707 — IC50 = 1000.0 nM 6.00
CHEMBL373773 — IC50 = 1100.0 nM 5.96
CHEMBL218999 — IC50 = 1100.0 nM 5.96
CHEMBL220195 — IC50 = 1100.0 nM 5.96
CHEMBL441864 — IC50 = 1200.0 nM 5.92
CHEMBL218894 — IC50 = 1200.0 nM 5.92
CHEMBL218847 — IC50 = 1300.0 nM 5.89
CHEMBL374634 — IC50 = 1400.0 nM 5.85
CHEMBL387117 — IC50 = 1400.0 nM 5.85
CHEMBL219703 — IC50 = 1500.0 nM 5.82
CHEMBL441864 — IC50 = 1600.0 nM 5.80
CHEMBL218193 — IC50 = 1700.0 nM 5.77
CHEMBL219703 — IC50 = 1700.0 nM 5.77
CHEMBL374769 — IC50 = 1800.0 nM 5.75
CHEMBL219224 — IC50 = 1900.0 nM 5.72
CHEMBL219653 — IC50 = 2100.0 nM 5.68
CHEMBL219335 — IC50 = 2100.0 nM 5.68
CHEMBL387117 — IC50 = 2400.0 nM 5.62
CHEMBL376852 — IC50 = 2400.0 nM 5.62
CHEMBL217975 — IC50 = 2600.0 nM 5.58
CHEMBL217975 — IC50 = 2700.0 nM 5.57
CHEMBL218847 — IC50 = 2900.0 nM 5.54
CHEMBL218849 — IC50 = 3300.0 nM 5.48
CHEMBL218848 — IC50 = 3300.0 nM 5.48
CHEMBL218894 — IC50 = 3500.0 nM 5.46
CHEMBL218849 — IC50 = 4000.0 nM 5.40
CHEMBL376852 — IC50 = 4100.0 nM 5.39
CHEMBL375118 — IC50 = 4200.0 nM 5.38
CHEMBL375118 — IC50 = 4600.0 nM 5.34
CHEMBL219224 — IC50 = 4700.0 nM 5.33
CHEMBL218193 — IC50 = 4700.0 nM 5.33
CHEMBL373773 — IC50 = 4700.0 nM 5.33
CHEMBL796 METHYLPHENIDATE IC50 = 5100.0 nM 5.29
CHEMBL219653 — IC50 = 5600.0 nM 5.25
CHEMBL219707 — IC50 = 6400.0 nM 5.19
CHEMBL373710 — IC50 = 7300.0 nM 5.14
CHEMBL219334 — IC50 > 9600.0 nM -
CHEMBL219116 — IC50 > 10000000.0 nM -
CHEMBL373710 — IC50 > 8300.0 nM -