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Assay Detail

CHEMBL1819644

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

Binding
Displacement of [3H]WIN-35428 from human recombinant DAT by scintillation proximity assay
44
Total Activities
39
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-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: further insights into a class of triple re-uptake inhibitors.
Micheli F, Cavanni P, Bettati M, Bonanomi G, Di Fabio R, Fazzolari E, Marchioro C, Roscic M, Tarsi L, Visentini F, Zonzini L, Worby A.
Bioorg Med Chem (2011) 19 : 3451 -3461
PubMed 21550808 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 7.95 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1818444 1 9.80
CHEMBL1818445 2 9.70
CHEMBL296602 INDATRALINE 2.0 1 9.10
CHEMBL1818447 1 9.10
CHEMBL1818443 1 9.00
CHEMBL1818461 1 8.90
CHEMBL1818456 1 8.80
CHEMBL1818460 1 8.70
CHEMBL1818446 1 8.70
CHEMBL1818455 2 8.50
CHEMBL1818452 2 8.50
CHEMBL1818547 1 8.40
CHEMBL1818454 1 8.20
CHEMBL1818448 1 8.20
CHEMBL1818462 1 8.20
CHEMBL1818468 1 8.10
CHEMBL608151 1 8.10
CHEMBL1173532 GSK1360707 1.0 1 8.00
CHEMBL1818450 1 7.90
CHEMBL1818465 1 7.90
CHEMBL1818464 1 7.90
CHEMBL1173607 1 7.90
CHEMBL1818451 2 7.80
CHEMBL1818441 1 7.80
CHEMBL1818543 2 7.80
CHEMBL1818463 1 7.80
CHEMBL1818458 1 7.70
CHEMBL1818467 1 7.70
CHEMBL1818546 1 7.70
CHEMBL1818459 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1818444 Ki = 0.1585 nM 9.80
CHEMBL1818445 Ki = 0.1995 nM 9.70
CHEMBL296602 INDATRALINE Ki = 0.7943 nM 9.10
CHEMBL1818447 Ki = 0.7943 nM 9.10
CHEMBL1818443 Ki = 1.0 nM 9.00
CHEMBL1818461 Ki = 1.259 nM 8.90
CHEMBL1818456 Ki = 1.585 nM 8.80
CHEMBL1818446 Ki = 1.995 nM 8.70
CHEMBL1818460 Ki = 1.995 nM 8.70
CHEMBL1818455 Ki = 3.162 nM 8.50
CHEMBL1818452 Ki = 3.162 nM 8.50
CHEMBL1818547 Ki = 3.981 nM 8.40
CHEMBL1818462 Ki = 6.31 nM 8.20
CHEMBL1818454 Ki = 6.31 nM 8.20
CHEMBL1818448 Ki = 6.31 nM 8.20
CHEMBL608151 Ki = 7.943 nM 8.10
CHEMBL1818468 Ki = 7.943 nM 8.10
CHEMBL1173532 GSK1360707 Ki = 10.0 nM 8.00
CHEMBL1818465 Ki = 12.59 nM 7.90
CHEMBL1818464 Ki = 12.59 nM 7.90
CHEMBL1818450 Ki = 12.59 nM 7.90
CHEMBL1173607 Ki = 12.59 nM 7.90
CHEMBL1818543 Ki = 15.85 nM 7.80
CHEMBL1818463 Ki = 15.85 nM 7.80
CHEMBL1818451 Ki = 15.85 nM 7.80
CHEMBL1818441 Ki = 15.85 nM 7.80
CHEMBL1818546 Ki = 19.95 nM 7.70
CHEMBL1818467 Ki = 19.95 nM 7.70
CHEMBL1818445 Ki = 19.95 nM 7.70
CHEMBL1818458 Ki = 19.95 nM 7.70
CHEMBL1818459 Ki = 25.12 nM 7.60
CHEMBL1818457 Ki = 25.12 nM 7.60
CHEMBL1818542 Ki = 25.12 nM 7.60
CHEMBL1818545 Ki = 25.12 nM 7.60
CHEMBL1818466 Ki = 31.62 nM 7.50
CHEMBL1818544 Ki = 63.1 nM 7.20
CHEMBL1818449 Ki = 63.1 nM 7.20
CHEMBL1818442 AMITIFADINE HYDROCHLORIDE Ki = 79.43 nM 7.10
CHEMBL1818452 Ki = 100.0 nM 7.00
CHEMBL1818453 Ki = 125.89 nM 6.90
CHEMBL1818455 Ki = 158.49 nM 6.80
CHEMBL1818469 Ki = 199.53 nM 6.70
CHEMBL1818543 Ki = 199.53 nM 6.70
CHEMBL1818451 Ki = 316.23 nM 6.50