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Assay Detail

CHEMBL808910

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)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 16 7.42 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339863 1 8.30
CHEMBL337929 1 8.11
CHEMBL127365 1 8.01
CHEMBL339281 1 7.95
CHEMBL126019 1 7.90
CHEMBL340816 1 7.81
CHEMBL338469 1 7.80
CHEMBL127013 1 7.73
CHEMBL126742 1 7.49
CHEMBL405524 1 7.22
CHEMBL339712 1 7.13
CHEMBL338411 1 6.93
CHEMBL125795 1 6.76
CHEMBL127790 1 6.58
CHEMBL126762 1 6.56
CHEMBL127180 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339863 Ki = 4.95 nM 8.30
CHEMBL337929 Ki = 7.71 nM 8.11
CHEMBL127365 Ki = 9.87 nM 8.01
CHEMBL339281 Ki = 11.28 nM 7.95
CHEMBL126019 Ki = 12.7 nM 7.90
CHEMBL340816 Ki = 15.36 nM 7.81
CHEMBL338469 Ki = 15.87 nM 7.80
CHEMBL127013 Ki = 18.8 nM 7.73
CHEMBL126742 Ki = 32.7 nM 7.49
CHEMBL405524 Ki = 60.8 nM 7.22
CHEMBL339712 Ki = 73.33 nM 7.13
CHEMBL338411 Ki = 118.0 nM 6.93
CHEMBL125795 Ki = 175.0 nM 6.76
CHEMBL127790 Ki = 260.1 nM 6.58
CHEMBL126762 Ki = 275.1 nM 6.56
CHEMBL127180 Ki = 357.3 nM 6.45