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Compound Detail

CHEMBL3702341

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Cc1c(C(=O)NCCCN(C)C)sc2ncnc(Nc3ccc(F)cc3OC(C)CF)c12

Basic Information

ChEMBL ID CHEMBL3702341
Phase Preclinical
Structure Type MOL
InChI Key WTCFYBGLEUOJNE-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
17
Publications
0
Known Names

Molecular Properties

463.6
MW (Da)
4.30
ALogP
7
HBA
2
HBD
79.4
PSA (Ų)
0.44
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H27F2N5O2S
MW 463.55
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -2.04

Activity Summary

IC50 5 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
IC50 8.15 7.9167 7.0 3
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
IC50 7.64 7.64 23.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724801 Fibroblast 320
- 10.6019/CHEMBL5724801 U2OS 320
- 10.6019/CHEMBL5724801 HEK-293T 320
- 10.6019/CHEMBL5303304 HEK-293T 8
30496989 10.1016/j.ejmech.2018.10.070 Unchecked 6
30496989 10.1016/j.ejmech.2018.10.070 MAP kinase-interacting serine/threonine-protein kinase 2 5
30496989 10.1016/j.ejmech.2018.10.070 MAP kinase-interacting serine/threonine-protein kinase 1 4
37669595 10.1016/j.ejmech.2023.115781 MAP kinase-interacting serine/threonine-protein kinase 1 3
- 10.6019/CHEMBL5303304 Fibroblast 3
30496989 10.1016/j.ejmech.2018.10.070 MAP kinase-interacting serine/threonine-protein kinase 1/2 2
33892273 10.1016/j.ejmech.2021.113420 MAP kinase-interacting serine/threonine-protein kinase 2 1
37669595 10.1016/j.ejmech.2023.115781 MAP kinase-interacting serine/threonine-protein kinase 2 1
- 10.6019/CHEMBL5303304 U2OS 1
33892273 10.1016/j.ejmech.2021.113420 MAP kinase-interacting serine/threonine-protein kinase 1 1
30496989 10.1016/j.ejmech.2018.10.070 3T3-L1 1
30496989 10.1016/j.ejmech.2018.10.070 MDA-MB-231 1
30496989 10.1016/j.ejmech.2018.10.070 Mitogen-activated protein kinase 1 and 3 (ERK2 and ERK1) 1

Data from ChEMBL 36 via Core Engine