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Assay Detail

CHEMBL808909

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

Binding
Sigma 2 binding assay was done rat liver membrane, by labeling the binding site with [3H]DTG (DuPont-NEN) in the presence of [3H](+)-pentazocine (100 nM)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 3 — Cell-line / Tissue
Curated By Expert

Publication

N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4'-piperidine]: vesamicol analogues with affinity for monoamine transporters.
Efange SM, Kamath AP, Khare AB, Kung MP, Mach RH, Parsons SM.
J Med Chem (1997) 40 : 3905 -3914
PubMed 9397171 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.43 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL341139 1 8.48
CHEMBL340185 1 8.06
CHEMBL338140 1 7.64
CHEMBL315146 1 7.52
CHEMBL20730 VESAMICOL 1 7.47
CHEMBL87414 1 7.17
CHEMBL126257 1 7.00
CHEMBL340815 1 6.86
CHEMBL314170 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL341139 Ki = 3.3 nM 8.48
CHEMBL340185 Ki = 8.8 nM 8.06
CHEMBL338140 Ki = 22.9 nM 7.64
CHEMBL315146 Ki = 30.0 nM 7.52
CHEMBL20730 VESAMICOL Ki = 34.0 nM 7.47
CHEMBL87414 Ki = 67.0 nM 7.17
CHEMBL126257 Ki = 99.2 nM 7.00
CHEMBL340815 Ki = 139.2 nM 6.86
CHEMBL314170 Ki = 224.0 nM 6.65