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Compound Detail

CHEMBL5205822

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O=C(Cc1cccc(C(F)(F)F)c1)Nc1cc(Oc2cc3nc(NC(=O)C4CC4)sc3cc2F)ccc1F

Basic Information

ChEMBL ID CHEMBL5205822
Phase Preclinical
Structure Type MOL
InChI Key AVPUTQITOHDIOV-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

547.5
MW (Da)
6.92
ALogP
5
HBA
2
HBD
80.3
PSA (Ų)
0.25
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H18F5N3O3S
MW 547.51
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -2.15

Activity Summary

Kd 2 meas. best 7.11
EC50 1 meas. best 6.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-interacting serine/threonine-protein kinase 3
CHEMBL1795199
Kd 7.11 7.11 77.0 1
Receptor-interacting serine/threonine-protein kinase 1
CHEMBL5464
Kd 7.01 7.01 97.0 1
HT-29
CHEMBL384
EC50 6.77 6.77 170.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36288088 10.1021/acs.jmedchem.2c01478 HT-29 2
36288088 10.1021/acs.jmedchem.2c01478 Receptor-interacting serine/threonine-protein kinase 1 1
36288088 10.1021/acs.jmedchem.2c01478 Receptor-interacting serine/threonine-protein kinase 3 1

Data from ChEMBL 36 via Core Engine