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Assay Detail

CHEMBL923872

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

Binding
Displacement of [125I]RTI55 from DAT in rat brain synaptosomes
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Synaptosomes
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

DAT/SERT selectivity of flexible GBR 12909 analogs modeled using 3D-QSAR methods.
Gilbert KM, Boos TL, Dersch CM, Greiner E, Jacobson AE, Lewis D, Matecka D, Prisinzano TE, Zhang Y, Rothman RB, Rice KC, Venanzi CA.
Bioorg Med Chem (2007) 15 : 1146 -1159
PubMed 17127069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 8.11 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160073 1 9.15
CHEMBL416409 1 9.15
CHEMBL538405 1 9.14
CHEMBL429492 1 9.10
CHEMBL286991 1 9.05
CHEMBL136154 1 9.00
CHEMBL409161 1 8.96
CHEMBL35122 1 8.96
CHEMBL36141 1 8.92
CHEMBL34591 1 8.92
CHEMBL290799 1 8.92
CHEMBL28660 1 8.89
CHEMBL255065 1 8.89
CHEMBL137020 1 8.79
CHEMBL284096 1 8.68
CHEMBL36419 1 8.64
CHEMBL281594 VANOXERINE 3.0 1 8.43
CHEMBL159445 1 8.39
CHEMBL429840 1 8.32
CHEMBL136249 1 8.28
CHEMBL285673 1 8.24
CHEMBL164270 1 8.19
CHEMBL28897 1 8.19
CHEMBL35045 1 8.10
CHEMBL163272 1 8.10
CHEMBL252759 1 8.03
CHEMBL34032 1 8.00
CHEMBL289013 1 7.88
CHEMBL286949 1 7.85
CHEMBL35411 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160073 Ki = 0.7 nM 9.15
CHEMBL416409 Ki = 0.71 nM 9.15
CHEMBL538405 Ki = 0.73 nM 9.14
CHEMBL429492 Ki = 0.8 nM 9.10
CHEMBL286991 Ki = 0.9 nM 9.05
CHEMBL136154 Ki = 1.01 nM 9.00
CHEMBL409161 Ki = 1.1 nM 8.96
CHEMBL35122 Ki = 1.1 nM 8.96
CHEMBL36141 Ki = 1.2 nM 8.92
CHEMBL34591 Ki = 1.2 nM 8.92
CHEMBL290799 Ki = 1.2 nM 8.92
CHEMBL28660 Ki = 1.3 nM 8.89
CHEMBL255065 Ki = 1.3 nM 8.89
CHEMBL137020 Ki = 1.61 nM 8.79
CHEMBL284096 Ki = 2.1 nM 8.68
CHEMBL36419 Ki = 2.3 nM 8.64
CHEMBL281594 VANOXERINE Ki = 3.7 nM 8.43
CHEMBL159445 Ki = 4.1 nM 8.39
CHEMBL429840 Ki = 4.77 nM 8.32
CHEMBL136249 Ki = 5.3 nM 8.28
CHEMBL285673 Ki = 5.7 nM 8.24
CHEMBL164270 Ki = 6.4 nM 8.19
CHEMBL28897 Ki = 6.4 nM 8.19
CHEMBL163272 Ki = 8.0 nM 8.10
CHEMBL35045 Ki = 7.9 nM 8.10
CHEMBL252759 Ki = 9.32 nM 8.03
CHEMBL34032 Ki = 9.9 nM 8.00
CHEMBL289013 Ki = 13.3 nM 7.88
CHEMBL286949 Ki = 14.0 nM 7.85
CHEMBL35411 Ki = 16.0 nM 7.80
CHEMBL164297 Ki = 16.1 nM 7.79
CHEMBL255054 Ki = 18.0 nM 7.75
CHEMBL403575 Ki = 20.0 nM 7.70
CHEMBL27748 Ki = 22.0 nM 7.66
CHEMBL159982 Ki = 31.0 nM 7.51
CHEMBL252758 Ki = 33.7 nM 7.47
CHEMBL400707 Ki = 40.0 nM 7.40
CHEMBL251242 Ki = 42.0 nM 7.38
CHEMBL28935 Ki = 49.0 nM 7.31
CHEMBL28414 Ki = 53.0 nM 7.28
CHEMBL434093 Ki = 56.0 nM 7.25
CHEMBL28867 Ki = 57.0 nM 7.24
CHEMBL163163 Ki = 61.8 nM 7.21
CHEMBL34372 Ki = 63.0 nM 7.20
CHEMBL255055 Ki = 64.6 nM 7.19
CHEMBL29000 Ki = 84.0 nM 7.08
CHEMBL28726 Ki = 87.0 nM 7.06
CHEMBL254843 Ki = 100.0 nM 7.00