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Compound Detail

CHEMBL4862473

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O=C(C1CC1)N1CCN(Cc2nc3ccccc3n2Cc2cccc(C(F)(F)F)c2)CC1

Basic Information

ChEMBL ID CHEMBL4862473
Phase Preclinical
Structure Type MOL
InChI Key RGZUYPIISREBSF-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

442.5
MW (Da)
4.16
ALogP
4
HBA
0
HBD
41.4
PSA (Ų)
0.60
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 C24H25F3N4O
MW 442.49
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -2.03

Activity Summary

IC50 5 meas. best 6.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinaldehyde dehydrogenase 3
CHEMBL3579
IC50 6.23 6.23 590.0 1
Aldehyde dehydrogenase 1A1
CHEMBL3577
IC50 6.04 6.04 921.0 1
Retinal dehydrogenase 2
CHEMBL3112384
IC50 5.86 5.86 1370.0 1
Aldehyde dehydrogenase, mitochondrial
CHEMBL1935
IC50 5.66 5.66 2170.0 1
Aldehyde dehydrogenase, dimeric NADP-preferring
CHEMBL3578
IC50 5.58 5.58 2620.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.104 mL.min-1.g-1 Homo sapiens
T1/2 0.45 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34403955 10.1016/j.bmc.2021.116352 HepG2 5
34403955 10.1016/j.bmc.2021.116352 ADMET 4
34403955 10.1016/j.bmc.2021.116352 Aldehyde dehydrogenase 1A1 2
34403955 10.1016/j.bmc.2021.116352 Retinal dehydrogenase 2 1
34403955 10.1016/j.bmc.2021.116352 Retinaldehyde dehydrogenase 3 1
34403955 10.1016/j.bmc.2021.116352 Aldehyde dehydrogenase, mitochondrial 1
34403955 10.1016/j.bmc.2021.116352 Aldehyde dehydrogenase, dimeric NADP-preferring 1

Data from ChEMBL 36 via Core Engine