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Compound Detail

CHEMBL557138

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C=C(Br)C(=O)Nc1cc(C(=O)Nc2cc(C(=O)Nc3cc(C(=O)Nc4cc(C(=O)NCCc5ncc[nH]5)n(C)c4)n(C)c3)n(C)c2)n(C)c1.Cl

Basic Information

ChEMBL ID CHEMBL557138
Phase Preclinical
Structure Type MOL
InChI Key PXMLFSQJAUJBJZ-UHFFFAOYSA-N
Parent Compound CHEMBL1196468
Active Moiety CHEMBL1196468
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

732.6
MW (Da)
3.34
ALogP
10
HBA
6
HBD
193.9
PSA (Ų)
0.11
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H35BrClN11O5
MW 769.06
Aromatic Rings 5
Heavy Atoms 49
NP-Likeness -0.71

Activity Summary

IC50 1 meas. best 8.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L1210
CHEMBL386
IC50 8.61 8.61 2.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
L1210 IC50 = 2.46 nM 8.61 In vitro test for cytotoxicity against L1210 murine leukemia cells 15115402

Literature References

PubMed DOI Target Context # Activities
10866398 10.1016/s0960-894x(00)00205-5 Mus musculus 2
15115402 10.1021/jm031051k L1210 1
10866398 10.1016/s0960-894x(00)00205-5 L1210 1

Data from ChEMBL 36 via Core Engine