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Assay Detail

CHEMBL911118

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

Binding
Displacement of [125I]RTI-55 from human DAT expressing HEK293 cells
ChEMBL ↗
55
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 dopamine transporter (CHEMBL238) ↗
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
Ki 55 7.04 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219649 — — 2 9.01
CHEMBL218999 — — 2 9.00
CHEMBL220195 — — 2 8.85
CHEMBL374634 — — 2 8.64
CHEMBL373710 — — 2 8.44
CHEMBL219335 — — 2 8.43
CHEMBL387117 — — 2 8.18
CHEMBL218849 — — 2 8.11
CHEMBL219653 — — 2 8.03
CHEMBL218847 — — 2 7.96
CHEMBL220247 — — 2 7.80
CHEMBL217975 — — 2 7.66
CHEMBL219703 — — 2 7.64
CHEMBL219281 — — 2 7.62
CHEMBL219116 — — 2 7.60
CHEMBL375118 — — 2 7.44
CHEMBL376852 — — 2 7.43
CHEMBL218848 — — 2 7.34
CHEMBL218894 — — 2 7.28
CHEMBL796 METHYLPHENIDATE 4.0 1 6.96
CHEMBL374769 — — 2 6.92
CHEMBL219707 — — 2 6.89
CHEMBL219224 — — 2 6.75
CHEMBL219540 — — 1 6.43
CHEMBL219334 — — 2 6.40
CHEMBL441864 — — 2 6.36
CHEMBL373773 — — 2 6.36
CHEMBL370805 COCAINE 4.0 1 6.30
CHEMBL218193 — — 2 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219649 — Ki = 0.97 nM 9.01
CHEMBL218999 — Ki = 1.0 nM 9.00
CHEMBL220195 — Ki = 1.4 nM 8.85
CHEMBL374634 — Ki = 2.3 nM 8.64
CHEMBL373710 — Ki = 3.6 nM 8.44
CHEMBL219335 — Ki = 3.7 nM 8.43
CHEMBL387117 — Ki = 6.6 nM 8.18
CHEMBL218849 — Ki = 7.8 nM 8.11
CHEMBL219653 — Ki = 9.4 nM 8.03
CHEMBL218847 — Ki = 11.0 nM 7.96
CHEMBL220247 — Ki = 16.0 nM 7.80
CHEMBL217975 — Ki = 22.0 nM 7.66
CHEMBL219703 — Ki = 23.0 nM 7.64
CHEMBL219281 — Ki = 24.0 nM 7.62
CHEMBL219116 — Ki = 25.0 nM 7.60
CHEMBL374634 — Ki = 29.0 nM 7.54
CHEMBL218999 — Ki = 31.0 nM 7.51
CHEMBL375118 — Ki = 36.0 nM 7.44
CHEMBL376852 — Ki = 37.0 nM 7.43
CHEMBL219649 — Ki = 43.0 nM 7.37
CHEMBL387117 — Ki = 44.0 nM 7.36
CHEMBL218848 — Ki = 46.0 nM 7.34
CHEMBL218894 — Ki = 52.0 nM 7.28
CHEMBL220195 — Ki = 90.0 nM 7.05
CHEMBL796 METHYLPHENIDATE Ki = 110.0 nM 6.96
CHEMBL374769 — Ki = 120.0 nM 6.92
CHEMBL219707 — Ki = 130.0 nM 6.89
CHEMBL219335 — Ki = 140.0 nM 6.85
CHEMBL220247 — Ki = 170.0 nM 6.77
CHEMBL219224 — Ki = 180.0 nM 6.75
CHEMBL219707 — Ki = 260.0 nM 6.58
CHEMBL218849 — Ki = 290.0 nM 6.54
CHEMBL219653 — Ki = 310.0 nM 6.51
CHEMBL219540 — Ki = 370.0 nM 6.43
CHEMBL218847 — Ki = 380.0 nM 6.42
CHEMBL219334 — Ki = 400.0 nM 6.40
CHEMBL373773 — Ki = 440.0 nM 6.36
CHEMBL441864 — Ki = 440.0 nM 6.36
CHEMBL370805 COCAINE Ki = 500.0 nM 6.30
CHEMBL373710 — Ki = 510.0 nM 6.29
CHEMBL373773 — Ki = 550.0 nM 6.26
CHEMBL374769 — Ki = 600.0 nM 6.22
CHEMBL375118 — Ki = 690.0 nM 6.16
CHEMBL219281 — Ki = 700.0 nM 6.16
CHEMBL218894 — Ki = 770.0 nM 6.11
CHEMBL219703 — Ki = 870.0 nM 6.06
CHEMBL218848 — Ki = 900.0 nM 6.05
CHEMBL217975 — Ki = 950.0 nM 6.02
CHEMBL376852 — Ki = 1800.0 nM 5.75
CHEMBL219116 — Ki = 2000.0 nM 5.70