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Assay Detail

CHEMBL679110

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Binding
Binding affinity towards dopamine transporter (DAT)
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter.
Lewis D, Zhang Y, Prisinzano T, Dersch CM, Rothman RB, Jacobson AE, Rice KC.
Bioorg Med Chem Lett (2003) 13 : 1385 -1389
PubMed 12657288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 51 7.50 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286991 1 9.05
CHEMBL28660 1 8.89
CHEMBL417660 1 8.68
CHEMBL10914 1 8.60
CHEMBL26320 1 8.43
CHEMBL281594 VANOXERINE 3.0 1 8.43
CHEMBL29286 1 8.41
CHEMBL421862 1 8.39
CHEMBL28821 1 8.21
CHEMBL28897 1 8.19
CHEMBL28712 1 8.14
CHEMBL286949 1 8.14
CHEMBL28236 1 8.12
CHEMBL285566 1 8.00
CHEMBL28414 1 7.85
CHEMBL28598 1 7.82
CHEMBL29003 1 7.75
CHEMBL29040 1 7.75
CHEMBL31571 1 7.72
CHEMBL27748 1 7.66
CHEMBL416198 1 7.66
CHEMBL28505 1 7.50
CHEMBL28133 1 7.50
CHEMBL416022 1 7.46
CHEMBL283646 1 7.43
CHEMBL29151 1 7.43
CHEMBL28947 1 7.42
CHEMBL28876 1 7.41
CHEMBL283620 1 7.40
CHEMBL283662 1 7.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286991 Ki = 0.9 nM 9.05
CHEMBL28660 Ki = 1.3 nM 8.89
CHEMBL417660 Ki = 2.1 nM 8.68
CHEMBL10914 Ki = 2.5 nM 8.60
CHEMBL26320 Ki = 3.7 nM 8.43
CHEMBL281594 VANOXERINE Ki = 3.7 nM 8.43
CHEMBL29286 Ki = 3.9 nM 8.41
CHEMBL421862 Ki = 4.1 nM 8.39
CHEMBL28821 Ki = 6.1 nM 8.21
CHEMBL28897 Ki = 6.4 nM 8.19
CHEMBL28712 Ki = 7.2 nM 8.14
CHEMBL286949 Ki = 7.3 nM 8.14
CHEMBL28236 Ki = 7.5 nM 8.12
CHEMBL285566 Ki = 10.0 nM 8.00
CHEMBL28414 Ki = 14.0 nM 7.85
CHEMBL28598 Ki = 15.0 nM 7.82
CHEMBL29003 Ki = 18.0 nM 7.75
CHEMBL29040 Ki = 18.0 nM 7.75
CHEMBL31571 Ki = 19.0 nM 7.72
CHEMBL27748 Ki = 22.0 nM 7.66
CHEMBL416198 Ki = 22.0 nM 7.66
CHEMBL28505 Ki = 32.0 nM 7.50
CHEMBL28133 Ki = 32.0 nM 7.50
CHEMBL416022 Ki = 35.0 nM 7.46
CHEMBL29151 Ki = 37.0 nM 7.43
CHEMBL283646 Ki = 37.0 nM 7.43
CHEMBL28947 Ki = 38.0 nM 7.42
CHEMBL28876 Ki = 39.0 nM 7.41
CHEMBL283620 Ki = 40.0 nM 7.40
CHEMBL283662 Ki = 48.0 nM 7.32
CHEMBL28935 Ki = 49.0 nM 7.31
CHEMBL28867 Ki = 57.0 nM 7.24
CHEMBL29065 Ki = 59.0 nM 7.23
CHEMBL28726 Ki = 62.0 nM 7.21
CHEMBL416752 Ki = 72.0 nM 7.14
CHEMBL28907 Ki = 78.0 nM 7.11
CHEMBL29000 Ki = 84.0 nM 7.08
CHEMBL31361 Ki = 84.0 nM 7.08
CHEMBL282312 Ki = 89.0 nM 7.05
CHEMBL28191 Ki = 170.0 nM 6.77
CHEMBL283837 Ki = 190.0 nM 6.72
CHEMBL417305 Ki = 210.0 nM 6.68
CHEMBL430537 Ki = 210.0 nM 6.68
CHEMBL27907 Ki = 208.0 nM 6.68
CHEMBL28125 Ki = 250.0 nM 6.60
CHEMBL27626 Ki = 260.0 nM 6.58
CHEMBL282821 Ki = 270.0 nM 6.57
CHEMBL28306 Ki = 290.0 nM 6.54
CHEMBL30257 Ki = 300.0 nM 6.52
CHEMBL281669 Ki = 390.0 nM 6.41