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Assay Detail

CHEMBL3100690

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

Binding
Displacement of [3H]DTG from guinea pig brain sigma2 receptor after 120 mins by scintillation counting analysis in presence of SKF10,047
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

From NMDA receptor antagonists to discovery of selective σ₂ receptor ligands.
Gitto R, De Luca L, Ferro S, Scala A, Ronsisvalle S, Parenti C, Prezzavento O, Buemi MR, Chimirri A.
Bioorg Med Chem (2014) 22 : 393 -397
PubMed 24290063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.47 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099036 1 8.12
CHEMBL3099037 1 8.00
CHEMBL456206 1 8.00
CHEMBL54 HALOPERIDOL 4.0 1 7.89
CHEMBL305187 IFENPRODIL 2.0 1 7.73
CHEMBL3099034 1 7.70
CHEMBL3099035 1 7.68
CHEMBL3099052 1 7.33
CHEMBL3099053 1 7.24
CHEMBL518480 1 7.12
CHEMBL3099050 1 6.65
CHEMBL3099051 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099036 Ki = 7.5 nM 8.12
CHEMBL3099037 Ki = 10.0 nM 8.00
CHEMBL456206 Ki = 10.0 nM 8.00
CHEMBL54 HALOPERIDOL Ki = 13.0 nM 7.89
CHEMBL305187 IFENPRODIL Ki = 18.8 nM 7.73
CHEMBL3099034 Ki = 20.0 nM 7.70
CHEMBL3099035 Ki = 21.0 nM 7.68
CHEMBL3099052 Ki = 47.0 nM 7.33
CHEMBL3099053 Ki = 57.0 nM 7.24
CHEMBL518480 Ki = 76.5 nM 7.12
CHEMBL3099050 Ki = 224.0 nM 6.65
CHEMBL3099051 Ki = 658.0 nM 6.18