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Assay Detail

CHEMBL4675313

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

Binding
Agonist activity at human DOR expressed in CHO cell membranes incubated for 60 mins scintillation counting assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14- O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives.
Spetea M,Rief SB,Haddou TB,Fink M,Kristeva E,Mittendorfer H,Haas S,Hummer N,Follia V,Guerrieri E,Asim MF,Sturm S,Schmidhammer H
J Med Chem (2019) 62 : 641 -653
PubMed 30571123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 8.17 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4754944 1 9.41
CHEMBL4795312 1 9.32
CHEMBL4741203 1 8.95
CHEMBL4789014 1 8.94
CHEMBL4795517 1 8.89
CHEMBL4792012 1 8.81
CHEMBL4783612 1 8.77
CHEMBL4753934 1 8.75
CHEMBL4788003 1 8.66
CHEMBL4781006 1 8.65
CHEMBL4755067 1 8.60
CHEMBL4754111 1 8.55
CHEMBL4760163 1 8.50
CHEMBL4750229 1 8.45
CHEMBL4763225 1 8.40
CHEMBL4740918 1 8.34
CHEMBL4763643 1 8.28
CHEMBL4780909 1 8.26
CHEMBL4782629 1 8.24
CHEMBL4740464 1 8.22
CHEMBL4745745 1 8.21
CHEMBL4788604 1 8.16
CHEMBL4755501 1 8.11
CHEMBL4755734 1 8.10
CHEMBL4757240 1 8.08
CHEMBL1672084 1 8.02
CHEMBL4782642 1 8.02
CHEMBL4761784 1 8.01
CHEMBL4740360 1 8.00
CHEMBL4761211 1 7.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4754944 EC50 = 0.39 nM 9.41
CHEMBL4795312 EC50 = 0.48 nM 9.32
CHEMBL4741203 EC50 = 1.12 nM 8.95
CHEMBL4789014 EC50 = 1.16 nM 8.94
CHEMBL4795517 EC50 = 1.3 nM 8.89
CHEMBL4792012 EC50 = 1.56 nM 8.81
CHEMBL4783612 EC50 = 1.71 nM 8.77
CHEMBL4753934 EC50 = 1.76 nM 8.75
CHEMBL4788003 EC50 = 2.18 nM 8.66
CHEMBL4781006 EC50 = 2.22 nM 8.65
CHEMBL4755067 EC50 = 2.52 nM 8.60
CHEMBL4754111 EC50 = 2.84 nM 8.55
CHEMBL4760163 EC50 = 3.18 nM 8.50
CHEMBL4750229 EC50 = 3.57 nM 8.45
CHEMBL4763225 EC50 = 3.96 nM 8.40
CHEMBL4740918 EC50 = 4.6 nM 8.34
CHEMBL4763643 EC50 = 5.2 nM 8.28
CHEMBL4780909 EC50 = 5.46 nM 8.26
CHEMBL4782629 EC50 = 5.73 nM 8.24
CHEMBL4740464 EC50 = 6.06 nM 8.22
CHEMBL4745745 EC50 = 6.23 nM 8.21
CHEMBL4788604 EC50 = 6.98 nM 8.16
CHEMBL4755501 EC50 = 7.8 nM 8.11
CHEMBL4755734 EC50 = 7.92 nM 8.10
CHEMBL4757240 EC50 = 8.36 nM 8.08
CHEMBL1672084 EC50 = 9.61 nM 8.02
CHEMBL4782642 EC50 = 9.55 nM 8.02
CHEMBL4761784 EC50 = 9.78 nM 8.01
CHEMBL4740360 EC50 = 10.1 nM 8.00
CHEMBL4761211 EC50 = 10.8 nM 7.97
CHEMBL4747179 EC50 = 11.8 nM 7.93
CHEMBL4741308 EC50 = 13.9 nM 7.86
CHEMBL4757463 EC50 = 20.1 nM 7.70
CHEMBL4748047 EC50 = 20.5 nM 7.69
CHEMBL4777389 EC50 = 24.3 nM 7.61
CHEMBL4793953 EC50 = 33.8 nM 7.47
CHEMBL4743953 EC50 = 34.4 nM 7.46
CHEMBL607405 EC50 = 37.3 nM 7.43
CHEMBL4741873 EC50 = 45.1 nM 7.35
CHEMBL4776879 EC50 = 96.4 nM 7.02
CHEMBL4797321 EC50 = 98.2 nM 7.01
CHEMBL4793888 EC50 = 152.0 nM 6.82