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Assay Detail

CHEMBL1056549

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

ADMET
Inhibition of human CYP2D6 by fluorescence-based assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cytochrome P450 2D6 (CHEMBL289)
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
IC50 32 5.44 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL551412 1 7.05
CHEMBL550063 1 6.36
CHEMBL550669 1 6.19
CHEMBL563137 1 6.17
CHEMBL551536 1 6.00
CHEMBL551413 1 5.92
CHEMBL551613 1 5.75
CHEMBL550472 1 5.68
CHEMBL563700 1 5.66
CHEMBL556439 1 5.62
CHEMBL563893 1 5.58
CHEMBL561805 1 5.55
CHEMBL551615 1 5.55
CHEMBL550471 1 5.51
CHEMBL561882 1 5.39
CHEMBL494462 1 5.37
CHEMBL550261 1 5.36
CHEMBL562478 1 5.34
CHEMBL564922 1 5.33
CHEMBL562873 1 5.28
CHEMBL562898 1 5.24
CHEMBL557121 1 5.21
CHEMBL556648 1 5.15
CHEMBL551414 1 5.12
CHEMBL559414 1 5.12
CHEMBL557257 1 5.02
CHEMBL557458 1 5.02
CHEMBL562280 1 4.68
CHEMBL557054 1 4.52
CHEMBL561138 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL551412 IC50 = 89.0 nM 7.05
CHEMBL550063 IC50 = 440.0 nM 6.36
CHEMBL550669 IC50 = 640.0 nM 6.19
CHEMBL563137 IC50 = 670.0 nM 6.17
CHEMBL551536 IC50 = 1000.0 nM 6.00
CHEMBL551413 IC50 = 1200.0 nM 5.92
CHEMBL551613 IC50 = 1800.0 nM 5.75
CHEMBL550472 IC50 = 2100.0 nM 5.68
CHEMBL563700 IC50 = 2200.0 nM 5.66
CHEMBL556439 IC50 = 2400.0 nM 5.62
CHEMBL563893 IC50 = 2600.0 nM 5.58
CHEMBL561805 IC50 = 2800.0 nM 5.55
CHEMBL551615 IC50 = 2800.0 nM 5.55
CHEMBL550471 IC50 = 3100.0 nM 5.51
CHEMBL561882 IC50 = 4100.0 nM 5.39
CHEMBL494462 IC50 = 4300.0 nM 5.37
CHEMBL550261 IC50 = 4400.0 nM 5.36
CHEMBL562478 IC50 = 4600.0 nM 5.34
CHEMBL564922 IC50 = 4700.0 nM 5.33
CHEMBL562873 IC50 = 5300.0 nM 5.28
CHEMBL562898 IC50 = 5700.0 nM 5.24
CHEMBL557121 IC50 = 6200.0 nM 5.21
CHEMBL556648 IC50 = 7100.0 nM 5.15
CHEMBL551414 IC50 = 7600.0 nM 5.12
CHEMBL559414 IC50 = 7500.0 nM 5.12
CHEMBL557257 IC50 = 9500.0 nM 5.02
CHEMBL557458 IC50 = 9500.0 nM 5.02
CHEMBL562280 IC50 = 21000.0 nM 4.68
CHEMBL557054 IC50 = 30000.0 nM 4.52
CHEMBL561138 IC50 = 33000.0 nM 4.48
CHEMBL561339 ADL-5747 FREE BASE IC50 = 43000.0 nM 4.37
CHEMBL556923 IC50 - -