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Assay Detail

CHEMBL2050136

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

Binding
Displacement of [3H]DTG from sigma2 receptor in rat liver homogenate after 120 mins by liquid scintillation counting in presence of (+)-pentazocine
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
Tu Z, Wang W, Cui J, Zhang X, Lu X, Xu J, Parsons SM.
Bioorg Med Chem (2012) 20 : 4422 -4429
PubMed 22739089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 5.12 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20730 VESAMICOL 1 6.46
CHEMBL2047120 1 5.86
CHEMBL2047127 1 5.59
CHEMBL2047122 1 5.40
CHEMBL2047124 1 5.40
CHEMBL2047126 1 5.38
CHEMBL2047232 1 5.31
CHEMBL2047234 1 5.20
CHEMBL2047238 1 5.11
CHEMBL2047239 1 5.01
CHEMBL2047237 1 4.91
CHEMBL2047123 1 4.81
CHEMBL2047125 1 4.79
CHEMBL2047240 1 4.69
CHEMBL2047236 1 4.68
CHEMBL2047235 1 4.61
CHEMBL2047233 1 4.61
CHEMBL2047128 1 4.39
CHEMBL2047121 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20730 VESAMICOL Ki = 346.0 nM 6.46
CHEMBL2047120 Ki = 1375.0 nM 5.86
CHEMBL2047127 Ki = 2590.0 nM 5.59
CHEMBL2047122 Ki = 3950.0 nM 5.40
CHEMBL2047124 Ki = 4000.0 nM 5.40
CHEMBL2047126 Ki = 4220.0 nM 5.38
CHEMBL2047232 Ki = 4850.0 nM 5.31
CHEMBL2047234 Ki = 6380.0 nM 5.20
CHEMBL2047238 Ki = 7830.0 nM 5.11
CHEMBL2047239 Ki = 9709.0 nM 5.01
CHEMBL2047237 Ki = 12300.0 nM 4.91
CHEMBL2047123 Ki = 15500.0 nM 4.81
CHEMBL2047125 Ki = 16400.0 nM 4.79
CHEMBL2047240 Ki = 20500.0 nM 4.69
CHEMBL2047236 Ki = 20700.0 nM 4.68
CHEMBL2047235 Ki = 24400.0 nM 4.61
CHEMBL2047233 Ki = 24300.0 nM 4.61
CHEMBL2047128 Ki = 40400.0 nM 4.39
CHEMBL2047121 Ki > 10000.0 nM -