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Compound Detail

CHEMBL5423332

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CN1CCN(c2ccnc(C(=O)N3CC[C@H](C(=O)Nc4cccc(-c5ccc(C(N)=O)cc5)c4)C3)c2)CC1

Basic Information

ChEMBL ID CHEMBL5423332
Phase Preclinical
Structure Type MOL
InChI Key KRLKMNVGYCKTTM-QHCPKHFHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

512.6
MW (Da)
2.70
ALogP
6
HBA
2
HBD
111.9
PSA (Ų)
0.53
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H32N6O3
MW 512.61
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.82

Activity Summary

IC50 1 meas. best 5.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TP53-binding protein 1
CHEMBL2424509
IC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
TP53-binding protein 1 IC50 = 2200.0 nM 5.66 Displacement of Biotin-p53K381acK382me2 from N-terminal his6-tagged 53BP1 (1484 ... 37782247

Literature References

PubMed DOI Target Context # Activities
37782247 10.1021/acs.jmedchem.3c01192 TP53-binding protein 1 1

Data from ChEMBL 36 via Core Engine