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Assay Detail

CHEMBL2039328

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

Binding
Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver after 180 mins by solid scintillation counting in the presence of (+)-pentazocine
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Microwave assisted synthesis of spirocyclic pyrrolidines -σ1 receptor ligands with modified benzene-N-distance.
Jasper A, Schepmann D, Lehmkuhl K, Vela JM, Buschmann H, Holenz J, Wünsch B.
Eur J Med Chem (2012) 53 : 327 -336
PubMed 22578786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.47 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282433 DITOLYLGUANIDINE 1 7.38
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL2035281 1 7.08
CHEMBL2035279 1 6.90
CHEMBL2034985 1 6.54
CHEMBL2035276 1 6.37
CHEMBL2035282 1 6.34
CHEMBL2035280 1 6.02
CHEMBL577956 1 5.99
CHEMBL2035277 1 5.93
CHEMBL141209 1 5.46
CHEMBL2035278 1 -
CHEMBL2035283 1 -
CHEMBL2035275 1 -
CHEMBL2035274 1 -
CHEMBL2035273 1 -
CHEMBL2035258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282433 DITOLYLGUANIDINE Ki = 42.0 nM 7.38
CHEMBL54 HALOPERIDOL Ki = 78.0 nM 7.11
CHEMBL2035281 Ki = 84.0 nM 7.08
CHEMBL2035279 Ki = 127.0 nM 6.90
CHEMBL2034985 Ki = 290.0 nM 6.54
CHEMBL2035276 Ki = 428.0 nM 6.37
CHEMBL2035282 Ki = 453.0 nM 6.34
CHEMBL2035280 Ki = 964.0 nM 6.02
CHEMBL577956 Ki = 1020.0 nM 5.99
CHEMBL2035277 Ki = 1180.0 nM 5.93
CHEMBL141209 Ki = 3500.0 nM 5.46
CHEMBL2035278 Ki > 1000.0 nM -
CHEMBL2035283 Ki > 1000.0 nM -
CHEMBL2035275 Ki > 1000.0 nM -
CHEMBL2035274 Ki > 1000.0 nM -
CHEMBL2035273 Ki > 1500.0 nM -
CHEMBL2035258 Ki > 1500.0 nM -