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Assay Detail

CHEMBL855089

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

Binding
Inhibition of DAT
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity.
Watson PS, Jiang B, Harrison K, Asakawa N, Welch PK, Covington M, Stowell NC, Wadman EA, Davies P, Solomon KA, Newton RC, Trainor GL, Friedman SM, Decicco CP, Ko SS.
Bioorg Med Chem Lett (2006) 16 : 5695 -5699
PubMed 16931001 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.51 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL218997 2 8.00
CHEMBL220766 1 7.51
CHEMBL218581 1 7.50
CHEMBL218174 1 7.02
CHEMBL217987 1 6.92
CHEMBL386073 1 6.80
CHEMBL219048 1 6.66
CHEMBL220819 1 6.60
CHEMBL218262 1 6.53
CHEMBL218568 1 6.35
CHEMBL384199 1 6.21
CHEMBL220765 1 6.21
CHEMBL220713 1 6.19
CHEMBL376737 1 6.12
CHEMBL221067 1 6.12
CHEMBL221903 1 6.07
CHEMBL386493 1 6.03
CHEMBL383879 1 5.91
CHEMBL384649 1 5.68
CHEMBL220801 1 5.65
CHEMBL385607 1 5.58
CHEMBL217928 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL218997 Ki = 10.0 nM 8.00
CHEMBL220766 Ki = 31.0 nM 7.51
CHEMBL218581 Ki = 32.0 nM 7.50
CHEMBL218997 Ki = 34.0 nM 7.47
CHEMBL218174 Ki = 96.0 nM 7.02
CHEMBL217987 Ki = 119.0 nM 6.92
CHEMBL386073 Ki = 157.0 nM 6.80
CHEMBL219048 Ki = 219.0 nM 6.66
CHEMBL220819 Ki = 251.0 nM 6.60
CHEMBL218262 Ki = 297.0 nM 6.53
CHEMBL218568 Ki = 451.0 nM 6.35
CHEMBL384199 Ki = 609.0 nM 6.21
CHEMBL220765 Ki = 621.0 nM 6.21
CHEMBL220713 Ki = 651.0 nM 6.19
CHEMBL376737 Ki = 754.0 nM 6.12
CHEMBL221067 Ki = 756.0 nM 6.12
CHEMBL221903 Ki = 855.0 nM 6.07
CHEMBL386493 Ki = 931.0 nM 6.03
CHEMBL383879 Ki = 1224.0 nM 5.91
CHEMBL384649 Ki = 2082.0 nM 5.68
CHEMBL220801 Ki = 2240.0 nM 5.65
CHEMBL385607 Ki = 2659.0 nM 5.58
CHEMBL217928 Ki - -