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Compound Detail

CHEMBL5170448

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C=CC(=O)N(C)CCOc1c(-c2ccc(CN3CCN(CC(C)C)CC3=O)c(C)c2)ccnc1N

Basic Information

ChEMBL ID CHEMBL5170448
Phase Preclinical
Structure Type MOL
InChI Key KSVWWTYXHRFDJA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

479.6
MW (Da)
2.96
ALogP
6
HBA
1
HBD
92.0
PSA (Ų)
0.53
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H37N5O3
MW 479.63
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.82

Activity Summary

IC50 2 meas. best 9.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 9.16 9.16 0.7 1
Unchecked
CHEMBL612545
IC50 6.44 6.44 360.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 334.0 mL.min-1.kg-1 Homo sapiens
CL 793.0 mL.min-1.kg-1 Rattus norvegicus
Fu 0.29 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35041943 10.1016/j.bmcl.2022.128549 ADMET 3
35041943 10.1016/j.bmcl.2022.128549 Tyrosine-protein kinase BTK 2
35041943 10.1016/j.bmcl.2022.128549 Unchecked 1

Data from ChEMBL 36 via Core Engine