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Assay Detail

CHEMBL915241

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

Binding
Displacement of [3H]DTG rom guinea pig brain sigma 2 receptor
25
Total Activities
25
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

Novel sigma receptor ligands: synthesis and biological profile.
Prezzavento O, Campisi A, Ronsisvalle S, Li Volti G, Marrazzo A, Bramanti V, Cannavò G, Vanella L, Cagnotto A, Mennini T, Ientile R, Ronsisvalle G.
J Med Chem (2007) 50 : 951 -961
PubMed 17328523 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.76 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL375499 1 8.05
CHEMBL374686 1 8.05
CHEMBL225516 1 7.92
CHEMBL222236 1 7.88
CHEMBL426724 1 7.85
CHEMBL222235 1 7.75
CHEMBL222445 1 7.72
CHEMBL221348 1 7.47
CHEMBL282433 DITOLYLGUANIDINE 1 7.31
CHEMBL222301 1 7.29
CHEMBL385795 1 7.28
CHEMBL60542 (+)-PENTAZOCINE 1 5.81
CHEMBL386002 1 5.66
CHEMBL222307 1 5.62
CHEMBL221347 1 5.57
CHEMBL222394 1 5.47
CHEMBL374814 1 5.45
CHEMBL222736 1 5.20
CHEMBL222287 IBOGAINE 2.0 1 5.03
CHEMBL386931 1 -
CHEMBL222444 1 -
CHEMBL221370 1 -
CHEMBL373686 1 -
CHEMBL434385 1 -
CHEMBL225653 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL375499 Ki = 9.0 nM 8.05
CHEMBL374686 Ki = 8.9 nM 8.05
CHEMBL225516 Ki = 11.9 nM 7.92
CHEMBL222236 Ki = 13.2 nM 7.88
CHEMBL426724 Ki = 14.0 nM 7.85
CHEMBL222235 Ki = 18.0 nM 7.75
CHEMBL222445 Ki = 19.0 nM 7.72
CHEMBL221348 Ki = 34.0 nM 7.47
CHEMBL282433 DITOLYLGUANIDINE Ki = 49.0 nM 7.31
CHEMBL222301 Ki = 50.8 nM 7.29
CHEMBL385795 Ki = 53.0 nM 7.28
CHEMBL60542 (+)-PENTAZOCINE Ki = 1540.0 nM 5.81
CHEMBL386002 Ki = 2173.0 nM 5.66
CHEMBL222307 Ki = 2399.0 nM 5.62
CHEMBL221347 Ki = 2713.0 nM 5.57
CHEMBL222394 Ki = 3362.0 nM 5.47
CHEMBL374814 Ki = 3586.0 nM 5.45
CHEMBL222736 Ki = 6293.0 nM 5.20
CHEMBL222287 IBOGAINE Ki = 9310.0 nM 5.03
CHEMBL386931 Ki > 10000.0 nM -
CHEMBL222444 Ki > 10000.0 nM -
CHEMBL221370 Ki > 10000.0 nM -
CHEMBL373686 Ki > 10000.0 nM -
CHEMBL434385 Ki > 10000.0 nM -
CHEMBL225653 Ki > 10000.0 nM -