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Compound Detail

CHEMBL4847784

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O=C(NC1COC1)c1cc(-n2ncc3cc(Nc4ccccc4Cl)c(F)cc32)cs1

Basic Information

ChEMBL ID CHEMBL4847784
Phase Preclinical
Structure Type MOL
InChI Key NVZWLMGDVMWXOW-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
2
PK Parameters
12
Publications
0
Known Names

Molecular Properties

442.9
MW (Da)
4.75
ALogP
6
HBA
2
HBD
68.2
PSA (Ų)
0.47
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 C21H16ClFN4O2S
MW 442.90
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.80

Activity Summary

IC50 4 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 7.85 7.85 14.0 1
Mitogen-activated protein kinase 14
CHEMBL260
IC50 6.4 6.4 400.0 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.98 5.98 1050.0 1
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 5.88 5.88 1330.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.533 hr Homo sapiens
T1/2 0.3333 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34676036 10.1021/acsmedchemlett.1c00334 Unchecked 3
34676036 10.1021/acsmedchemlett.1c00334 ADMET 2
34676036 10.1021/acsmedchemlett.1c00334 Mitogen-activated protein kinase 10 1
34676036 10.1021/acsmedchemlett.1c00334 Mitogen-activated protein kinase 8 1
34676036 10.1021/acsmedchemlett.1c00334 Mitogen-activated protein kinase 9 1
34676036 10.1021/acsmedchemlett.1c00334 Mitogen-activated protein kinase 14 1
34676036 10.1021/acsmedchemlett.1c00334 Voltage-gated inwardly rectifying potassium channel KCNH2 1
34676036 10.1021/acsmedchemlett.1c00334 Cytochrome P450 1A2 1
34676036 10.1021/acsmedchemlett.1c00334 Cytochrome P450 2C9 1
34676036 10.1021/acsmedchemlett.1c00334 Cytochrome P450 2D6 1
34676036 10.1021/acsmedchemlett.1c00334 Cytochrome P450 3A4 1
34676036 10.1021/acsmedchemlett.1c00334 SH-SY5Y 1

Data from ChEMBL 36 via Core Engine