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Assay Detail

CHEMBL808280

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

Binding
Affinity against Sigma opioid receptor type 2 using [3H]- DTG in rat liver membranes
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Asymmetric synthesis of 9-alkyl-2-benzyl-6,7-benzomorphans: characterization as novel sigma receptor ligands.
Carroll FI, Bai X, Dehghani A, Mascarella SW, Williams W, Bowen WD.
J Med Chem (1999) 42 : 4621 -4629
PubMed 10579824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.40 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL560 1 7.44
CHEMBL139900 1 6.94
CHEMBL140618 1 6.88
CHEMBL336235 1 6.88
CHEMBL141070 1 6.83
CHEMBL356486 1 6.72
CHEMBL423548 1 6.43
CHEMBL341874 1 6.32
CHEMBL143050 1 6.31
CHEMBL143585 1 6.23
CHEMBL143486 1 6.22
CHEMBL344813 1 6.12
CHEMBL143660 1 6.11
CHEMBL139774 1 6.07
CHEMBL346665 1 6.07
CHEMBL435046 1 6.03
CHEMBL60542 (+)-PENTAZOCINE 1 5.81
CHEMBL143103 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL560 Ki = 36.5 nM 7.44
CHEMBL139900 Ki = 115.0 nM 6.94
CHEMBL140618 Ki = 131.0 nM 6.88
CHEMBL336235 Ki = 133.0 nM 6.88
CHEMBL141070 Ki = 149.0 nM 6.83
CHEMBL356486 Ki = 192.0 nM 6.72
CHEMBL423548 Ki = 371.0 nM 6.43
CHEMBL341874 Ki = 478.0 nM 6.32
CHEMBL143050 Ki = 487.0 nM 6.31
CHEMBL143585 Ki = 587.0 nM 6.23
CHEMBL143486 Ki = 607.0 nM 6.22
CHEMBL344813 Ki = 759.0 nM 6.12
CHEMBL143660 Ki = 785.0 nM 6.11
CHEMBL139774 Ki = 850.0 nM 6.07
CHEMBL346665 Ki = 854.0 nM 6.07
CHEMBL435046 Ki = 944.0 nM 6.03
CHEMBL60542 (+)-PENTAZOCINE Ki = 1540.0 nM 5.81
CHEMBL143103 Ki = 1710.0 nM 5.77