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Assay Detail

CHEMBL1056544

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Functional
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).
Le Bourdonnec B, Windh RT, Leister LK, Zhou QJ, Ajello CW, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE.
J Med Chem (2009) 52 : 5685 -5702
PubMed 19694468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 6.94 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL556648 1 7.80
CHEMBL494462 1 7.72
CHEMBL563893 1 7.70
CHEMBL557121 1 7.68
CHEMBL557458 1 7.58
CHEMBL556439 1 7.55
CHEMBL551613 1 7.35
CHEMBL561882 1 7.33
CHEMBL562873 1 7.18
CHEMBL550472 1 7.16
CHEMBL561805 1 7.09
CHEMBL551412 1 7.05
CHEMBL562280 1 7.04
CHEMBL561339 ADL-5747 FREE BASE 2.0 1 7.03
CHEMBL550261 1 7.00
CHEMBL551536 1 7.00
CHEMBL550063 1 6.96
CHEMBL551413 1 6.96
CHEMBL557054 1 6.82
CHEMBL551615 1 6.72
CHEMBL564922 1 6.70
CHEMBL551414 1 6.62
CHEMBL561138 1 6.57
CHEMBL557257 1 6.51
CHEMBL562478 1 6.44
CHEMBL562898 1 6.43
CHEMBL550471 1 6.38
CHEMBL563137 1 6.35
CHEMBL563700 1 6.32
CHEMBL550669 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL556648 EC50 = 16.0 nM 7.80
CHEMBL494462 EC50 = 19.0 nM 7.72
CHEMBL563893 EC50 = 20.0 nM 7.70
CHEMBL557121 EC50 = 21.0 nM 7.68
CHEMBL557458 EC50 = 26.0 nM 7.58
CHEMBL556439 EC50 = 28.0 nM 7.55
CHEMBL551613 EC50 = 45.0 nM 7.35
CHEMBL561882 EC50 = 47.0 nM 7.33
CHEMBL562873 EC50 = 66.0 nM 7.18
CHEMBL550472 EC50 = 69.0 nM 7.16
CHEMBL561805 EC50 = 81.0 nM 7.09
CHEMBL551412 EC50 = 90.0 nM 7.05
CHEMBL562280 EC50 = 92.0 nM 7.04
CHEMBL561339 ADL-5747 FREE BASE EC50 = 94.0 nM 7.03
CHEMBL551536 EC50 = 100.0 nM 7.00
CHEMBL550261 EC50 = 100.0 nM 7.00
CHEMBL550063 EC50 = 110.0 nM 6.96
CHEMBL551413 EC50 = 110.0 nM 6.96
CHEMBL557054 EC50 = 150.0 nM 6.82
CHEMBL551615 EC50 = 190.0 nM 6.72
CHEMBL564922 EC50 = 200.0 nM 6.70
CHEMBL551414 EC50 = 240.0 nM 6.62
CHEMBL561138 EC50 = 270.0 nM 6.57
CHEMBL557257 EC50 = 310.0 nM 6.51
CHEMBL562478 EC50 = 360.0 nM 6.44
CHEMBL562898 EC50 = 370.0 nM 6.43
CHEMBL550471 EC50 = 420.0 nM 6.38
CHEMBL563137 EC50 = 450.0 nM 6.35
CHEMBL563700 EC50 = 480.0 nM 6.32
CHEMBL550669 EC50 = 980.0 nM 6.01
CHEMBL559414 EC50 = 980.0 nM 6.01
CHEMBL556923 EC50 - -