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Assay Detail

CHEMBL751664

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Binding
Ability to displace [3H]-deltorphin II from delta opioid receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Dermorphin tetrapeptide analogues with 2',6'-dimethylphenylalanine (Dmp) substituted for aromatic amino acids have high mu opioid receptor binding and biological activities.
Ambo A, Niizuma H, Sasaki A, Kohara H, Sasaki Y.
Bioorg Med Chem Lett (2003) 13 : 1269 -1272
PubMed 12657261 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.58 8.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23362 1 8.95
CHEMBL22321 1 6.32
CHEMBL23836 1 6.26
CHEMBL24059 1 5.77
CHEMBL280178 1 5.59
CHEMBL23133 1 -
CHEMBL23325 1 -
CHEMBL23295 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23362 Ki = 1.13 nM 8.95
CHEMBL22321 Ki = 482.0 nM 6.32
CHEMBL23836 Ki = 544.0 nM 6.26
CHEMBL24059 Ki = 1688.0 nM 5.77
CHEMBL280178 Ki = 2572.0 nM 5.59
CHEMBL23133 Ki > 2823.0 nM -
CHEMBL23325 Ki > 2823.0 nM -
CHEMBL23295 Ki > 2823.0 nM -