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Assay Detail

CHEMBL753952

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Binding
Ability to displace [3H]DAMGO from mu 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

Mu-type opioid receptor (CHEMBL270)
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 9.65 10.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24059 1 10.67
CHEMBL23836 1 10.46
CHEMBL23133 1 10.21
CHEMBL280178 1 10.21
CHEMBL22321 1 9.76
CHEMBL23325 1 8.14
CHEMBL23295 1 8.12
CHEMBL23362 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24059 Ki = 0.0216 nM 10.67
CHEMBL23836 Ki = 0.035 nM 10.46
CHEMBL23133 Ki = 0.0618 nM 10.21
CHEMBL280178 Ki = 0.0623 nM 10.21
CHEMBL22321 Ki = 0.172 nM 9.76
CHEMBL23325 Ki = 7.17 nM 8.14
CHEMBL23295 Ki = 7.62 nM 8.12
CHEMBL23362 Ki = 0.00205 nM -