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Assay Detail

CHEMBL915240

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

Binding
Displacement of [3H](+)-pentazocine from guinea pig brain sigma 1 receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 7.45 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL375499 1 9.17
CHEMBL225516 1 9.09
CHEMBL374686 1 9.01
CHEMBL426724 1 9.00
CHEMBL222301 1 8.82
CHEMBL222445 1 8.77
CHEMBL222235 1 8.72
CHEMBL222236 1 8.66
CHEMBL385795 1 8.51
CHEMBL60542 (+)-PENTAZOCINE 1 8.51
CHEMBL221348 1 8.51
CHEMBL282433 DITOLYLGUANIDINE 1 7.39
CHEMBL222287 IBOGAINE 2.0 1 6.60
CHEMBL221347 1 6.46
CHEMBL222394 1 6.45
CHEMBL386002 1 6.30
CHEMBL225653 1 6.21
CHEMBL222307 1 6.15
CHEMBL222444 1 6.11
CHEMBL386931 1 5.90
CHEMBL222736 1 5.88
CHEMBL434385 1 5.69
CHEMBL373686 1 5.51
CHEMBL221370 1 -
CHEMBL374814 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL375499 Ki = 0.68 nM 9.17
CHEMBL225516 Ki = 0.82 nM 9.09
CHEMBL374686 Ki = 0.97 nM 9.01
CHEMBL426724 Ki = 1.0 nM 9.00
CHEMBL222301 Ki = 1.5 nM 8.82
CHEMBL222445 Ki = 1.7 nM 8.77
CHEMBL222235 Ki = 1.9 nM 8.72
CHEMBL222236 Ki = 2.2 nM 8.66
CHEMBL385795 Ki = 3.1 nM 8.51
CHEMBL60542 (+)-PENTAZOCINE Ki = 3.1 nM 8.51
CHEMBL221348 Ki = 3.1 nM 8.51
CHEMBL282433 DITOLYLGUANIDINE Ki = 41.0 nM 7.39
CHEMBL222287 IBOGAINE Ki = 250.0 nM 6.60
CHEMBL221347 Ki = 350.0 nM 6.46
CHEMBL222394 Ki = 353.0 nM 6.45
CHEMBL386002 Ki = 497.0 nM 6.30
CHEMBL225653 Ki = 619.0 nM 6.21
CHEMBL222307 Ki = 707.0 nM 6.15
CHEMBL222444 Ki = 769.0 nM 6.11
CHEMBL386931 Ki = 1255.0 nM 5.90
CHEMBL222736 Ki = 1328.0 nM 5.88
CHEMBL434385 Ki = 2028.0 nM 5.69
CHEMBL373686 Ki = 3088.0 nM 5.51
CHEMBL221370 Ki > 10000.0 nM -
CHEMBL374814 Ki > 10000.0 nM -