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Assay Detail

CHEMBL1816474

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Binding
Inhibition of dopamine reuptake at DAT expressed in CHO-K1 cells
ChEMBL ↗
40
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues.
Shao L, Hewitt MC, Malcolm SC, Wang F, Ma J, Campbell UC, Spicer NA, Engel SR, Hardy LW, Jiang ZD, Schreiber R, Spear KL, Varney MA.
J Med Chem (2011) 54 : 5283 -5295
PubMed 21739935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 6.61 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1813317 — — 1 8.00
CHEMBL1813315 — — 1 7.85
CHEMBL1813313 — — 2 7.69
CHEMBL1813316 — — 1 7.60
CHEMBL1813485 — — 1 7.54
CHEMBL1813477 — — 1 7.52
CHEMBL273575 NOMIFENSINE 4.0 1 7.50
CHEMBL1813476 — — 1 7.47
CHEMBL1813478 — — 2 7.32
CHEMBL1813314 — — 1 7.26
CHEMBL1813470 — — 1 7.21
CHEMBL1813472 — — 1 7.08
CHEMBL1813483 — — 2 7.00
CHEMBL1813475 — — 1 6.91
CHEMBL1813474 — — 1 6.85
CHEMBL1813484 — — 1 6.83
CHEMBL1813489 — — 1 6.80
CHEMBL1813471 — — 2 6.69
CHEMBL1813308 — — 1 6.38
CHEMBL1813473 — — 2 6.34
CHEMBL1813487 — — 1 6.32
CHEMBL1813486 — — 1 6.31
CHEMBL1813488 — — 1 6.30
CHEMBL1813310 — — 1 6.00
CHEMBL1813306 — — 1 5.89
CHEMBL1813312 — — 2 5.88
CHEMBL1813307 — — 1 5.80
CHEMBL1813318 — — 1 5.61
CHEMBL1813479 — — 1 5.55
CHEMBL1813309 — — 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1813317 — IC50 = 10.0 nM 8.00
CHEMBL1813315 — IC50 = 14.13 nM 7.85
CHEMBL1813313 — IC50 = 20.42 nM 7.69
CHEMBL1813316 — IC50 = 25.12 nM 7.60
CHEMBL1813485 — IC50 = 28.84 nM 7.54
CHEMBL1813477 — IC50 = 30.2 nM 7.52
CHEMBL273575 NOMIFENSINE IC50 = 31.62 nM 7.50
CHEMBL1813476 — IC50 = 33.88 nM 7.47
CHEMBL1813478 — IC50 = 47.86 nM 7.32
CHEMBL1813314 — IC50 = 54.95 nM 7.26
CHEMBL1813470 — IC50 = 61.66 nM 7.21
CHEMBL1813478 — IC50 = 67.61 nM 7.17
CHEMBL1813472 — IC50 = 83.18 nM 7.08
CHEMBL1813483 — IC50 = 100.0 nM 7.00
CHEMBL1813475 — IC50 = 123.03 nM 6.91
CHEMBL1813474 — IC50 = 141.25 nM 6.85
CHEMBL1813484 — IC50 = 147.91 nM 6.83
CHEMBL1813489 — IC50 = 158.49 nM 6.80
CHEMBL1813483 — IC50 = 181.97 nM 6.74
CHEMBL1813471 — IC50 = 204.17 nM 6.69
CHEMBL1813313 — IC50 = 309.03 nM 6.51
CHEMBL1813308 — IC50 = 416.87 nM 6.38
CHEMBL1813473 — IC50 = 457.09 nM 6.34
CHEMBL1813471 — IC50 = 457.09 nM 6.34
CHEMBL1813487 — IC50 = 478.63 nM 6.32
CHEMBL1813486 — IC50 = 489.78 nM 6.31
CHEMBL1813488 — IC50 = 501.19 nM 6.30
CHEMBL1813310 — IC50 = 1000.0 nM 6.00
CHEMBL1813473 — IC50 = 1023.29 nM 5.99
CHEMBL1813306 — IC50 = 1288.25 nM 5.89
CHEMBL1813312 — IC50 = 1318.26 nM 5.88
CHEMBL1813307 — IC50 = 1584.89 nM 5.80
CHEMBL1813318 — IC50 = 2454.71 nM 5.61
CHEMBL1813479 — IC50 = 2818.38 nM 5.55
CHEMBL1813312 — IC50 = 3311.31 nM 5.48
CHEMBL1813309 — IC50 = 3388.44 nM 5.47
CHEMBL1813311 — IC50 = 9772.37 nM 5.01
CHEMBL1813482 — IC50 = 9772.37 nM 5.01
CHEMBL1813481 — IC50 > 10000.0 nM -
CHEMBL1813480 — IC50 > 10000.0 nM -