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Compound Detail

CHEMBL5798072

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CNCC(Cc1cccnc1)c1ccc2ccccc2c1

Basic Information

ChEMBL ID CHEMBL5798072
Phase Preclinical
Structure Type MOL
InChI Key ZBKRQGWGLHOYPX-UHFFFAOYSA-N
6
Targets
12
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

276.4
MW (Da)
3.78
ALogP
2
HBA
1
HBD
24.9
PSA (Ų)
0.77
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20N2
MW 276.38
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -0.17

Activity Summary

IC50 6 meas. best 6.24
Ki 6 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL228
Ki 8.64 8.255 2.3 2
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 8.42 8.205 3.8 2
Sodium-dependent dopamine transporter
CHEMBL238
Ki 7.11 7.035 78.0 2
Cytochrome P450 2D6
CHEMBL289
IC50 6.24 6.17 580.0 2
Cytochrome P450 3A4
CHEMBL340
IC50 5.09 4.955 8100.0 2
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.7 4.59 20000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium-dependent serotonin transporter Ki = 2.3 nM 8.64 Uptake Assay Protocol: SERT: This protocol was designed to measure inhibition of... -
Sodium-dependent noradrenaline transporter Ki = 3.8 nM 8.42 Uptake Assay Protocol: NET: This protocol was designed to measure inhibition of ... -
Sodium-dependent noradrenaline transporter Ki = 10.3 nM 7.99 Uptake Assay Protocol: NET: This protocol was designed to measure inhibition of ... -
Sodium-dependent serotonin transporter Ki = 13.6 nM 7.87 Uptake Assay Protocol: SERT: This protocol was designed to measure inhibition of... -
Sodium-dependent dopamine transporter Ki = 78.0 nM 7.11 Uptake Assay Protocol: DAT: This protocol was designed to measure inhibition of ... -
Sodium-dependent dopamine transporter Ki = 109.0 nM 6.96 Uptake Assay Protocol: DAT: This protocol was designed to measure inhibition of ... -
Cytochrome P450 2D6 IC50 = 580.0 nM 6.24 Inhibition Assay: Cytochrome P450 3A4 and 2D6:Recombinant enzymes, 3A4 and 2D6, ... -
Cytochrome P450 2D6 IC50 = 790.0 nM 6.1 Inhibition Assay: Cytochrome P450 3A4 and 2D6:Recombinant enzymes, 3A4 and 2D6, ... -
Cytochrome P450 3A4 IC50 = 8100.0 nM 5.09 Inhibition Assay: Cytochrome P450 3A4 and 2D6:Recombinant enzymes, 3A4 and 2D6, ... -
Cytochrome P450 3A4 IC50 = 15000.0 nM 4.82 Inhibition Assay: Cytochrome P450 3A4 and 2D6:Recombinant enzymes, 3A4 and 2D6, ... -
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 20000.0 nM 4.7 Activity Assay: HERG: The pre- and post-compound hERG current was evoked by a si... -
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 33000.0 nM 4.48 Activity Assay: HERG: The pre- and post-compound hERG current was evoked by a si... -

Data from ChEMBL 36 via Core Engine