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Assay Detail

CHEMBL882265

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

Binding
Inhibition of [3H]- 5-HT uptake in Serotonin transporter using serotonin uptake assay in rat midbrain tissue
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Midbrain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter.
Carroll FI, Kotian P, Dehghani A, Gray JL, Kuzemko MA, Parham KA, Abraham P, Lewin AH, Boja JW, Kuhar MJ.
J Med Chem (1995) 38 : 379 -388
PubMed 7830281 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.27 8.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14391 1 8.76
CHEMBL306208 1 8.30
CHEMBL82027 1 7.71
CHEMBL340761 1 7.29
CHEMBL2079586 1 7.00
CHEMBL127040 1 6.89
CHEMBL14144 1 6.41
CHEMBL340912 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14391 Ki = 1.74 nM 8.76
CHEMBL306208 Ki = 5.0 nM 8.30
CHEMBL82027 Ki = 19.38 nM 7.71
CHEMBL340761 Ki = 51.64 nM 7.29
CHEMBL2079586 Ki = 100.56 nM 7.00
CHEMBL127040 Ki = 128.62 nM 6.89
CHEMBL14144 Ki = 390.68 nM 6.41
CHEMBL340912 Ki = 1537.14 nM 5.81