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Compound Detail

CHEMBL4787487

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COC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N[N+](=O)[O-])NC(=O)CC/C(C)=C/Cc1c(O)c2c(c(C)c1OC)COC2=O)[C@@H](C)O

Basic Information

ChEMBL ID CHEMBL4787487
Phase Preclinical
Structure Type MOL
InChI Key DSRCRHHCECAYTF-BBDYVAIOSA-N
1
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

862.0
MW (Da)
-0.14
ALogP
15
HBA
9
HBD
327.0
PSA (Ų)
0.01
QED
3
Ro5 Violations
23
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H59N9O13
MW 861.95
Aromatic Rings 1
Heavy Atoms 61
NP-Likeness 0.65

Activity Summary

EC50 2 meas. best 4.45
IC50 2 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 4.45 4.45 35430.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 35430.0 nM 4.45 Immunosuppression-mediated antiproliferative activity against anti-CD3/anti-CD28... 32007665

Literature References

PubMed DOI Target Context # Activities
32007665 10.1016/j.ejmech.2020.112091 Unchecked 5
32007665 10.1016/j.ejmech.2020.112091 Jurkat 2
32007665 10.1016/j.ejmech.2020.112091 ADMET 1

Data from ChEMBL 36 via Core Engine