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Compound Detail

CHEMBL3799270

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COC(=O)Cc1cccc(NC(=O)C2(N(C)C)CCN(c3ncnc4[nH]c5c(c34)CC(F)(F)CC5)CC2)c1

Basic Information

ChEMBL ID CHEMBL3799270
Phase Preclinical
Structure Type MOL
InChI Key DTVFQHOXYKFHFO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

526.6
MW (Da)
3.34
ALogP
7
HBA
2
HBD
103.5
PSA (Ų)
0.48
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32F2N6O3
MW 526.59
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.84

Activity Summary

IC50 1 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
LIM domain kinase 2
CHEMBL5932
IC50 9.7 9.7 0.2 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.1667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
LIM domain kinase 2 IC50 = 0.2 nM 9.7 Inhibition of human LIMK2 using cofilin as substrate preincubated for 20 mins fo... -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C5MD00473J LIM domain kinase 2 1
- 10.1039/C5MD00473J Plasma 1

Data from ChEMBL 36 via Core Engine