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Assay Detail

CHEMBL756645

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

Binding
Binding affinity for Opioid receptor mu 1 by displacement of [3H]- DAGO
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.
Salvadori S, Balboni G, Guerrini R, Tomatis R, Bianchi C, Bryant SD, Cooper PS, Lazarus LH.
J Med Chem (1997) 40 : 3100 -3108
PubMed 9301674 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 5.38 6.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93041 1 6.56
CHEMBL104842 1 6.42
CHEMBL106853 1 6.29
CHEMBL107386 1 6.02
CHEMBL107644 1 5.88
CHEMBL2370386 1 5.82
CHEMBL107754 1 5.70
CHEMBL104436 1 5.61
CHEMBL3038229 1 5.59
CHEMBL571492 2 5.48
CHEMBL2370384 1 5.24
CHEMBL2370388 1 5.23
CHEMBL104705 1 4.94
CHEMBL104171 1 4.91
CHEMBL318395 1 4.88
CHEMBL2370390 1 4.72
CHEMBL2370387 1 4.72
CHEMBL485576 1 4.55
CHEMBL105263 1 4.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93041 Ki = 277.0 nM 6.56
CHEMBL104842 Ki = 379.4 nM 6.42
CHEMBL106853 Ki = 511.4 nM 6.29
CHEMBL107386 Ki = 954.9 nM 6.02
CHEMBL107644 Ki = 1329.0 nM 5.88
CHEMBL2370386 Ki = 1520.0 nM 5.82
CHEMBL107754 Ki = 2003.0 nM 5.70
CHEMBL104436 Ki = 2435.0 nM 5.61
CHEMBL3038229 Ki = 2555.0 nM 5.59
CHEMBL571492 Ki = 3320.0 nM 5.48
CHEMBL2370384 Ki = 5810.0 nM 5.24
CHEMBL2370388 Ki = 5853.0 nM 5.23
CHEMBL571492 Ki = 10962.0 nM 4.96
CHEMBL104705 Ki = 11523.0 nM 4.94
CHEMBL104171 Ki = 12386.0 nM 4.91
CHEMBL318395 Ki = 13089.0 nM 4.88
CHEMBL2370390 Ki = 18956.0 nM 4.72
CHEMBL2370387 Ki = 19210.0 nM 4.72
CHEMBL485576 Ki = 28411.0 nM 4.55
CHEMBL105263 Ki = 71373.0 nM 4.15