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Assay Detail

CHEMBL757321

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

Binding
Displacement of [3H]dihydromorphine (DHM) from rat brain Opioid receptors
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.
Bock MG, DiPardo RM, Evans BE, Rittle KE, Whitter WL, Veber DF, Freidinger RM, Chang RS, Chen TB, Lotti VJ.
J Med Chem (1990) 33 : 450 -455
PubMed 2153212 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.61 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL343066 1 9.52
CHEMBL140365 1 9.30
CHEMBL141354 1 8.52
CHEMBL337530 1 8.15
CHEMBL141629 1 7.75
CHEMBL342415 1 7.66
CHEMBL140749 1 7.52
CHEMBL141786 1 7.40
CHEMBL68870 1 7.30
CHEMBL141048 1 6.92
CHEMBL140620 1 6.35
CHEMBL334933 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL343066 IC50 = 0.3 nM 9.52
CHEMBL140365 IC50 = 0.5 nM 9.30
CHEMBL141354 IC50 = 3.0 nM 8.52
CHEMBL337530 IC50 = 7.0 nM 8.15
CHEMBL141629 IC50 = 18.0 nM 7.75
CHEMBL342415 IC50 = 22.0 nM 7.66
CHEMBL140749 IC50 = 30.0 nM 7.52
CHEMBL141786 IC50 = 40.0 nM 7.40
CHEMBL68870 IC50 = 50.0 nM 7.30
CHEMBL141048 IC50 = 120.0 nM 6.92
CHEMBL140620 IC50 = 450.0 nM 6.35
CHEMBL334933 IC50 = 12000.0 nM 4.92