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Compound Detail

CHEMBL5439842

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CCNC(=O)c1ccc2c([C@H]3CCN(CC4(O)CCOCC4)C[C@@H]3C)c(C)nn2c1

Basic Information

ChEMBL ID CHEMBL5439842
Phase Preclinical
Structure Type MOL
InChI Key SMHIDGFZIFNQKM-LPHOPBHVSA-N
2
Targets
4
Activities
3
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

414.6
MW (Da)
2.36
ALogP
6
HBA
2
HBD
79.1
PSA (Ų)
0.79
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H34N4O3
MW 414.55
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.72

Activity Summary

Ki 2 meas. best 7.43
IC50 1 meas. best 6.52
Kd 1 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
YEATS domain-containing protein 4
CHEMBL4296266
Kd 7.52 7.52 30.0 1
YEATS domain-containing protein 4
CHEMBL4296266
Ki 7.43 7.43 37.0 1
YEATS domain-containing protein 4
CHEMBL4296266
IC50 6.52 6.52 300.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
Ki 4.18 4.18 66600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36562986 10.1021/acs.jmedchem.2c01421 YEATS domain-containing protein 4 5
36562986 10.1021/acs.jmedchem.2c01421 Unchecked 4
36562986 10.1021/acs.jmedchem.2c01421 ADMET 2
36562986 10.1021/acs.jmedchem.2c01421 Voltage-gated inwardly rectifying potassium channel KCNH2 1
36562986 10.1021/acs.jmedchem.2c01421 No relevant target 1
36562986 10.1021/acs.jmedchem.2c01421 Bone marrow cell 1

Data from ChEMBL 36 via Core Engine