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Assay Detail

CHEMBL756572

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

Binding
Compound was evaluated for the binding affinity towards opioid receptor from rat whole brain using [3H]etorpine (33.2 Ci/mmol,0.2nanoM)as radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.
Ennis MD, Baze ME, Smith MW, Lawson CF, McCall RB, Lahti RA, Piercey MF.
J Med Chem (1992) 35 : 3058 -3066
PubMed 1323682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.53 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101535 1 10.00
CHEMBL320880 1 9.22
CHEMBL102175 1 8.51
CHEMBL323088 1 8.48
CHEMBL418802 1 8.37
CHEMBL318166 1 7.84
CHEMBL106283 1 6.88
CHEMBL103983 1 6.28
CHEMBL318374 1 6.12
CHEMBL319023 1 5.62
CHEMBL101483 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101535 Ki = 0.1 nM 10.00
CHEMBL320880 Ki = 0.6 nM 9.22
CHEMBL102175 Ki = 3.1 nM 8.51
CHEMBL323088 Ki = 3.3 nM 8.48
CHEMBL418802 Ki = 4.3 nM 8.37
CHEMBL318166 Ki = 14.4 nM 7.84
CHEMBL106283 Ki = 131.0 nM 6.88
CHEMBL103983 Ki = 530.0 nM 6.28
CHEMBL318374 Ki = 765.0 nM 6.12
CHEMBL319023 Ki = 2425.0 nM 5.62
CHEMBL101483 Ki = 3231.0 nM 5.49