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Assay Detail

CHEMBL4041092

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

Binding
Displacement of [3H]-imipramine from human serotonin transporter expressed in HEK-293 cell membranes after 30 mins by scintillation counting
37
Total Activities
37
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 serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.
Bucki A, Marcinkowska M, Śniecikowska J, Więckowski K, Pawłowski M, Głuch-Lutwin M, Gryboś A, Siwek A, Pytka K, Jastrzębska-Więsek M, Partyka A, Wesołowska A, Mierzejewski P, Kołaczkowski M.
J Med Chem (2017) 60 : 7483 -7501
PubMed 28763213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 8.32 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11 IMIPRAMINE 4.0 1 9.00
CHEMBL4075144 1 8.96
CHEMBL4071451 1 8.77
CHEMBL4104622 1 8.66
CHEMBL4075673 1 8.64
CHEMBL4091193 1 8.64
CHEMBL4092243 1 8.59
CHEMBL4104216 1 8.57
CHEMBL4084492 1 8.57
CHEMBL4070254 1 8.55
CHEMBL4087852 1 8.49
CHEMBL4066532 1 8.48
CHEMBL4080399 1 8.46
CHEMBL4095555 1 8.44
CHEMBL4100951 1 8.42
CHEMBL4080369 1 8.41
CHEMBL4077937 1 8.39
CHEMBL4066971 1 8.38
CHEMBL4062817 1 8.37
CHEMBL4103725 1 8.34
CHEMBL4069237 1 8.32
CHEMBL4065568 1 8.30
CHEMBL4096479 1 8.29
CHEMBL4074195 1 8.28
CHEMBL4088249 1 8.28
CHEMBL4060649 1 8.27
CHEMBL4095979 1 8.24
CHEMBL4085802 1 8.22
CHEMBL4077040 1 8.21
CHEMBL4070715 1 8.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11 IMIPRAMINE Ki = 1.0 nM 9.00
CHEMBL4075144 Ki = 1.1 nM 8.96
CHEMBL4071451 Ki = 1.7 nM 8.77
CHEMBL4104622 Ki = 2.2 nM 8.66
CHEMBL4075673 Ki = 2.3 nM 8.64
CHEMBL4091193 Ki = 2.3 nM 8.64
CHEMBL4092243 Ki = 2.6 nM 8.59
CHEMBL4104216 Ki = 2.7 nM 8.57
CHEMBL4084492 Ki = 2.7 nM 8.57
CHEMBL4070254 Ki = 2.8 nM 8.55
CHEMBL4087852 Ki = 3.2 nM 8.49
CHEMBL4066532 Ki = 3.3 nM 8.48
CHEMBL4080399 Ki = 3.5 nM 8.46
CHEMBL4095555 Ki = 3.6 nM 8.44
CHEMBL4100951 Ki = 3.8 nM 8.42
CHEMBL4080369 Ki = 3.9 nM 8.41
CHEMBL4077937 Ki = 4.1 nM 8.39
CHEMBL4066971 Ki = 4.2 nM 8.38
CHEMBL4062817 Ki = 4.3 nM 8.37
CHEMBL4103725 Ki = 4.6 nM 8.34
CHEMBL4069237 Ki = 4.8 nM 8.32
CHEMBL4065568 Ki = 5.0 nM 8.30
CHEMBL4096479 Ki = 5.1 nM 8.29
CHEMBL4074195 Ki = 5.2 nM 8.28
CHEMBL4088249 Ki = 5.3 nM 8.28
CHEMBL4060649 Ki = 5.4 nM 8.27
CHEMBL4095979 Ki = 5.7 nM 8.24
CHEMBL4085802 Ki = 6.0 nM 8.22
CHEMBL4077040 Ki = 6.2 nM 8.21
CHEMBL4070715 Ki = 6.1 nM 8.21
CHEMBL4078873 Ki = 8.5 nM 8.07
CHEMBL4067700 Ki = 12.0 nM 7.92
CHEMBL4088925 Ki = 16.0 nM 7.80
CHEMBL4099997 Ki = 18.0 nM 7.75
CHEMBL4079972 Ki = 25.0 nM 7.60
CHEMBL4104596 Ki = 32.0 nM 7.50
CHEMBL4081987 Ki = 40.0 nM 7.40