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Compound Detail

CHEMBL3355474

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C[C@@H]1COCCN1c1nc(-c2cncc3[nH]ccc23)cc2c1ncn2[C@@H](C)S(C)(=O)=O

Basic Information

ChEMBL ID CHEMBL3355474
Phase Preclinical
Structure Type MOL
InChI Key SSPHMGCXSJLCMP-ZIAGYGMSSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
17
Publications
0
Known Names

Molecular Properties

440.5
MW (Da)
2.76
ALogP
8
HBA
1
HBD
106.0
PSA (Ų)
0.52
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24N6O3S
MW 440.53
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.77

Activity Summary

IC50 2 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase ATR
CHEMBL5024
IC50 9.7 9.7 0.2 1
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 7.1 7.1 80.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 114.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25589928 10.1021/ml500352s ADMET 2
25589928 10.1021/ml500352s Cytochrome P450 1A2 2
25589928 10.1021/ml500352s Cytochrome P450 2C9 2
25589928 10.1021/ml500352s Cytochrome P450 2D6 2
25589928 10.1021/ml500352s Cytochrome P450 3A4 2
25589928 10.1021/ml500352s Serine/threonine-protein kinase mTOR 1
25589928 10.1021/ml500352s Rattus norvegicus 1
25589928 10.1021/ml500352s Voltage-gated inwardly rectifying potassium channel KCNH2 1
25589928 10.1021/ml500352s Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1
25589928 10.1021/ml500352s Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 1
25589928 10.1021/ml500352s Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 1
25589928 10.1021/ml500352s Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
25589928 10.1021/ml500352s DNA-dependent protein kinase catalytic subunit 1
25589928 10.1021/ml500352s Serine-protein kinase ATM 1
25589928 10.1021/ml500352s Serine/threonine-protein kinase ATR 1
25589928 10.1021/ml500352s Serine/threonine-protein kinase Chk1 1
25589928 10.1021/ml500352s No relevant target 1

Data from ChEMBL 36 via Core Engine