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Assay Detail

CHEMBL1068886

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

Binding
Displacement of [3H]WIN-35428 from human recombinant DAT expressed in BacMam virus-transduced cells by scintillation proximity assay
ChEMBL ↗
62
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors.
Micheli F, Cavanni P, Arban R, Benedetti R, Bertani B, Bettati M, Bettelini L, Bonanomi G, Braggio S, Checchia A, Davalli S, Di Fabio R, Fazzolari E, Fontana S, Marchioro C, Minick D, Negri M, Oliosi B, Read KD, Sartori I, Tedesco G, Tarsi L, Terreni S, Visentini F, Zocchi A, Zonzini L.
J Med Chem (2010) 53 : 2534 -2551
PubMed 20170186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 62 7.32 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596987 — — 2 8.60
CHEMBL611063 — — 1 8.40
CHEMBL596806 — — 1 8.30
CHEMBL605209 — — 1 8.30
CHEMBL596805 — — 1 8.20
CHEMBL611367 — — 1 8.20
CHEMBL590472 — — 1 8.20
CHEMBL608151 — — 2 8.10
CHEMBL602235 — — 2 8.10
CHEMBL598228 — — 1 8.10
CHEMBL598644 — — 1 8.00
CHEMBL602323 — — 1 8.00
CHEMBL608430 — — 1 7.90
CHEMBL610795 — — 1 7.90
CHEMBL598825 — — 1 7.90
CHEMBL609023 — — 1 7.80
CHEMBL2021582 — — 1 7.70
CHEMBL597000 — — 2 7.70
CHEMBL599845 — — 2 7.70
CHEMBL605119 — — 1 7.70
CHEMBL597190 — — 1 7.60
CHEMBL600645 — — 1 7.60
CHEMBL598215 — — 1 7.60
CHEMBL599639 — — 2 7.60
CHEMBL610220 — — 1 7.60
CHEMBL596796 — — 1 7.50
CHEMBL599241 — — 2 7.40
CHEMBL605502 — — 1 7.40
CHEMBL611379 — — 2 7.30
CHEMBL2021580 — — 2 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596987 — Ki = 2.512 nM 8.60
CHEMBL611063 — Ki = 3.981 nM 8.40
CHEMBL605209 — Ki = 5.012 nM 8.30
CHEMBL596806 — Ki = 5.012 nM 8.30
CHEMBL596805 — Ki = 6.31 nM 8.20
CHEMBL611367 — Ki = 6.31 nM 8.20
CHEMBL590472 — Ki = 6.31 nM 8.20
CHEMBL596987 — Ki = 6.31 nM 8.20
CHEMBL598228 — Ki = 7.943 nM 8.10
CHEMBL602235 — Ki = 7.943 nM 8.10
CHEMBL608151 — Ki = 7.943 nM 8.10
CHEMBL602323 — Ki = 10.0 nM 8.00
CHEMBL598644 — Ki = 10.0 nM 8.00
CHEMBL598825 — Ki = 12.59 nM 7.90
CHEMBL608430 — Ki = 12.59 nM 7.90
CHEMBL610795 — Ki = 12.59 nM 7.90
CHEMBL609023 — Ki = 15.85 nM 7.80
CHEMBL597000 — Ki = 19.95 nM 7.70
CHEMBL597000 — Ki = 19.95 nM 7.70
CHEMBL2021582 — Ki = 19.95 nM 7.70
CHEMBL599845 — Ki = 19.95 nM 7.70
CHEMBL605119 — Ki = 19.95 nM 7.70
CHEMBL599639 — Ki = 25.12 nM 7.60
CHEMBL610220 — Ki = 25.12 nM 7.60
CHEMBL600645 — Ki = 25.12 nM 7.60
CHEMBL597190 — Ki = 25.12 nM 7.60
CHEMBL608151 — Ki = 25.12 nM 7.60
CHEMBL598215 — Ki = 25.12 nM 7.60
CHEMBL596796 — Ki = 31.62 nM 7.50
CHEMBL599241 — Ki = 39.81 nM 7.40
CHEMBL605502 — Ki = 39.81 nM 7.40
CHEMBL598202 — Ki = 50.12 nM 7.30
CHEMBL603480 — Ki = 50.12 nM 7.30
CHEMBL2021580 — Ki = 50.12 nM 7.30
CHEMBL611379 — Ki = 50.12 nM 7.30
CHEMBL596809 — Ki = 56.23 nM 7.25
CHEMBL599242 — Ki = 63.1 nM 7.20
CHEMBL2021580 — Ki = 63.1 nM 7.20
CHEMBL597608 — Ki = 79.43 nM 7.10
CHEMBL598216 — Ki = 79.43 nM 7.10
CHEMBL599240 — Ki = 79.43 nM 7.10
CHEMBL599241 — Ki = 79.43 nM 7.10
CHEMBL596989 — Ki = 100.0 nM 7.00
CHEMBL596809 — Ki = 109.65 nM 6.96
CHEMBL592374 AMITIFADINE Ki = 125.89 nM 6.90
CHEMBL596795 — Ki = 125.89 nM 6.90
CHEMBL2021581 — Ki = 125.89 nM 6.90
CHEMBL599639 — Ki = 199.53 nM 6.70
CHEMBL488638 — Ki = 199.53 nM 6.70
CHEMBL2021577 — Ki = 199.53 nM 6.70