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Assay Detail

CHEMBL756653

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

Binding
Binding affinity against rat brain Opioid receptor mu 1 using [3H]DAMGO radioligand
32
Total Activities
32
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

Development of potent bifunctional endomorphin-2 analogues with mixed mu-/delta-opioid agonist and delta-opioid antagonist properties.
Fujita Y, Tsuda Y, Li T, Motoyama T, Takahashi M, Shimizu Y, Yokoi T, Sasaki Y, Ambo A, Kita A, Jinsmaa Y, Bryant SD, Lazarus LH, Okada Y.
J Med Chem (2004) 47 : 3591 -3599
PubMed 15214786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 8.52 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334147 1 9.96
CHEMBL120758 1 9.92
CHEMBL118942 1 9.89
CHEMBL331325 1 9.82
CHEMBL332371 1 9.77
CHEMBL433643 1 9.72
CHEMBL331255 1 9.66
CHEMBL339417 1 9.54
CHEMBL327036 1 9.48
CHEMBL409907 1 9.44
CHEMBL333350 1 9.31
CHEMBL332196 1 9.29
CHEMBL419591 1 9.28
CHEMBL333357 ENDOMORPHIN 2 1 9.16
CHEMBL120091 1 8.96
CHEMBL325702 1 8.62
CHEMBL119752 1 8.39
CHEMBL120023 1 8.24
CHEMBL120083 1 8.18
CHEMBL118681 1 7.88
CHEMBL331653 1 7.71
CHEMBL333007 1 7.67
CHEMBL120530 1 7.63
CHEMBL116708 1 7.58
CHEMBL120371 1 7.47
CHEMBL325230 1 7.33
CHEMBL326379 1 7.32
CHEMBL332309 1 7.31
CHEMBL332815 1 7.25
CHEMBL120410 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334147 Ki = 0.11 nM 9.96
CHEMBL120758 Ki = 0.12 nM 9.92
CHEMBL118942 Ki = 0.13 nM 9.89
CHEMBL331325 Ki = 0.15 nM 9.82
CHEMBL332371 Ki = 0.17 nM 9.77
CHEMBL433643 Ki = 0.19 nM 9.72
CHEMBL331255 Ki = 0.22 nM 9.66
CHEMBL339417 Ki = 0.29 nM 9.54
CHEMBL327036 Ki = 0.33 nM 9.48
CHEMBL409907 Ki = 0.36 nM 9.44
CHEMBL333350 Ki = 0.49 nM 9.31
CHEMBL332196 Ki = 0.51 nM 9.29
CHEMBL419591 Ki = 0.52 nM 9.28
CHEMBL333357 ENDOMORPHIN 2 Ki = 0.69 nM 9.16
CHEMBL120091 Ki = 1.11 nM 8.96
CHEMBL325702 Ki = 2.41 nM 8.62
CHEMBL119752 Ki = 4.07 nM 8.39
CHEMBL120023 Ki = 5.79 nM 8.24
CHEMBL120083 Ki = 6.59 nM 8.18
CHEMBL118681 Ki = 13.3 nM 7.88
CHEMBL331653 Ki = 19.6 nM 7.71
CHEMBL333007 Ki = 21.6 nM 7.67
CHEMBL120530 Ki = 23.6 nM 7.63
CHEMBL116708 Ki = 26.5 nM 7.58
CHEMBL120371 Ki = 33.5 nM 7.47
CHEMBL325230 Ki = 46.3 nM 7.33
CHEMBL326379 Ki = 48.2 nM 7.32
CHEMBL332309 Ki = 48.5 nM 7.31
CHEMBL332815 Ki = 55.8 nM 7.25
CHEMBL120410 Ki = 61.1 nM 7.21
CHEMBL330984 Ki = 72.9 nM 7.14
CHEMBL332523 Ki = 249.0 nM 6.60