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Compound Detail

CHEMBL4549229

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CCOC(=O)Nc1ccc(NCc2ccc(C(F)(F)F)nc2)c(F)c1N

Basic Information

ChEMBL ID CHEMBL4549229
Phase Preclinical
Structure Type MOL
InChI Key QGMYAHJROPECLZ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
9
Publications
0
Known Names

Molecular Properties

372.3
MW (Da)
4.00
ALogP
5
HBA
3
HBD
89.3
PSA (Ų)
0.55
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H16F4N4O2
MW 372.32
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.51

Activity Summary

EC50 3 meas. best 6.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Potassium voltage-gated channel subfamily KQT member 5
CHEMBL2925
EC50 6.27 6.27 540.0 1
Potassium voltage-gated channel subfamily KQT member 4
CHEMBL3576
EC50 6.18 6.18 660.0 1
Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3)
CHEMBL2221348
EC50 5.47 5.47 3360.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 6.767 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31223450 10.1021/acsmedchemlett.9b00097 Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) 1
31223450 10.1021/acsmedchemlett.9b00097 Voltage-gated potassium channel KCNQ3/KCNQ5 1
31223450 10.1021/acsmedchemlett.9b00097 Potassium voltage-gated channel subfamily KQT member 4 1
31223450 10.1021/acsmedchemlett.9b00097 KCNQ4/KCNQ5 1
31223450 10.1021/acsmedchemlett.9b00097 Unchecked 1
31223450 10.1021/acsmedchemlett.9b00097 ADMET 1
35671848 10.1016/j.bmcl.2022.128841 Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) 1
35671848 10.1016/j.bmcl.2022.128841 Potassium voltage-gated channel subfamily KQT member 4 1
35671848 10.1016/j.bmcl.2022.128841 Potassium voltage-gated channel subfamily KQT member 5 1

Data from ChEMBL 36 via Core Engine