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Assay Detail

CHEMBL1833396

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

Binding
Displacement of [3H]ditolylguanidine from rat liver sigma 2 receptor by scintillation counting
40
Total Activities
40
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

Combination of two pharmacophoric systems: synthesis and pharmacological evaluation of spirocyclic pyranopyrazoles with high σ₁ receptor affinity.
Schläger T, Schepmann D, Lehmkuhl K, Holenz J, Vela JM, Buschmann H, Wünsch B.
J Med Chem (2011) 54 : 6704 -6713
PubMed 21859078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 6.51 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1829565 1 7.40
CHEMBL282433 DITOLYLGUANIDINE 1 7.38
CHEMBL1171555 1 7.37
CHEMBL54 HALOPERIDOL 4.0 1 7.11
CHEMBL1829670 1 7.08
CHEMBL1170546 1 6.99
CHEMBL1829574 1 6.96
CHEMBL1829672 1 6.72
CHEMBL1829659 1 6.68
CHEMBL1829671 1 6.57
CHEMBL1829580 1 6.50
CHEMBL1829579 1 6.47
CHEMBL1829573 1 6.37
CHEMBL1829668 1 6.37
CHEMBL1829667 1 6.25
CHEMBL1829571 1 6.24
CHEMBL1829568 1 6.16
CHEMBL1829577 1 6.12
CHEMBL1829669 1 6.11
CHEMBL1829572 1 6.08
CHEMBL1829569 1 6.03
CHEMBL1829578 1 6.03
CHEMBL138809 1 5.89
CHEMBL141209 1 5.46
CHEMBL1829576 1 -
CHEMBL1829566 1 -
CHEMBL1829674 1 -
CHEMBL1829673 1 -
CHEMBL1170545 1 -
CHEMBL1829567 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1829565 Ki = 39.7 nM 7.40
CHEMBL282433 DITOLYLGUANIDINE Ki = 42.0 nM 7.38
CHEMBL1171555 Ki = 43.0 nM 7.37
CHEMBL54 HALOPERIDOL Ki = 78.0 nM 7.11
CHEMBL1829670 Ki = 83.0 nM 7.08
CHEMBL1170546 Ki = 102.0 nM 6.99
CHEMBL1829574 Ki = 109.0 nM 6.96
CHEMBL1829672 Ki = 191.0 nM 6.72
CHEMBL1829659 Ki = 209.0 nM 6.68
CHEMBL1829671 Ki = 269.0 nM 6.57
CHEMBL1829580 Ki = 316.0 nM 6.50
CHEMBL1829579 Ki = 340.0 nM 6.47
CHEMBL1829573 Ki = 428.0 nM 6.37
CHEMBL1829668 Ki = 429.0 nM 6.37
CHEMBL1829667 Ki = 557.0 nM 6.25
CHEMBL1829571 Ki = 570.0 nM 6.24
CHEMBL1829568 Ki = 687.0 nM 6.16
CHEMBL1829577 Ki = 752.0 nM 6.12
CHEMBL1829669 Ki = 773.0 nM 6.11
CHEMBL1829572 Ki = 833.0 nM 6.08
CHEMBL1829569 Ki = 925.0 nM 6.03
CHEMBL1829578 Ki = 933.0 nM 6.03
CHEMBL138809 Ki = 1280.0 nM 5.89
CHEMBL141209 Ki = 3500.0 nM 5.46
CHEMBL1829664 Ki > 1000.0 nM -
CHEMBL1829665 Ki > 1000.0 nM -
CHEMBL1829666 Ki > 1000.0 nM -
CHEMBL1829662 Ki > 1000.0 nM -
CHEMBL1829661 Ki > 1000.0 nM -
CHEMBL1829660 Ki > 1000.0 nM -
CHEMBL1829581 Ki > 1000.0 nM -
CHEMBL1829663 Ki > 1000.0 nM -
CHEMBL1829575 Ki > 1000.0 nM -
CHEMBL1829570 Ki > 1000.0 nM -
CHEMBL1829567 Ki > 1000.0 nM -
CHEMBL1170545 Ki > 1000.0 nM -
CHEMBL1829673 Ki > 1000.0 nM -
CHEMBL1829674 Ki > 1000.0 nM -
CHEMBL1829566 Ki > 1000.0 nM -
CHEMBL1829576 Ki > 1000.0 nM -