Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL3685796

MRL-SYKi
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
Cc1cc(Nc2nccc(C)n2)cc(-c2cnc([C@@]3(O)CC[C@H](C(=O)O)C(C)(C)C3)s2)c1

Basic Information

ChEMBL ID CHEMBL3685796
Name MRL-SYKi
Phase Preclinical
Structure Type MOL
InChI Key OYKPWSZSBLRRPL-HOYKHHGWSA-N
13
Targets
24
Activities
3
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

452.6
MW (Da)
5.06
ALogP
7
HBA
3
HBD
108.2
PSA (Ų)
0.50
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C24H28N4O3S
MW 452.58
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.45

Activity Summary

IC50 18 meas. best 9.05
Ki 5 meas. best 5.11
Kd 1 meas. best 8.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 9.05 8.388 0.9 5
Tyrosine-protein kinase SYK
CHEMBL2599
Kd 8.74 8.74 1.8 1
Tyrosine-protein kinase ZAP-70
CHEMBL2803
IC50 7.62 7.62 24.0 1
Mast cell
CHEMBL613709
IC50 7.42 7.42 38.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 7.0 7.0 100.0 2
High affinity nerve growth factor receptor
CHEMBL2815
IC50 6.98 6.98 105.0 2
NT-3 growth factor receptor
CHEMBL5608
IC50 6.92 6.92 120.0 2
Tyrosine-protein kinase Fgr
CHEMBL4454
IC50 6.73 6.73 185.0 1
Tyrosine-protein kinase Fyn
CHEMBL1841
IC50 6.69 6.69 205.0 1
Tyrosine-protein kinase Fer
CHEMBL3982
IC50 6.63 6.63 232.0 1
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 6.62 6.62 242.0 1
Cysteinyl leukotriene receptor
CHEMBL2094254
IC50 6.54 6.54 287.0 1
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 5.11 5.1067 7713.0 3
Histamine H3 receptor
CHEMBL264
Ki 5.0 5.0 10000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase SYK IC50 = 0.9 nM 9.05 Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000714a SYK -
Tyrosine-protein kinase SYK IC50 = 0.9 nM 9.05 Human SKY enzyme assay -
Tyrosine-protein kinase SYK IC50 = 1.0 nM 9.0 Homogeneous Time-Resolved Fluorescence (HTRF) Assay : A recombinant GST-hSYK fus... -
Tyrosine-protein kinase SYK Kd = 1.8 nM 8.74 KinomeScan assay: inhibition of SYK -
Tyrosine-protein kinase ZAP-70 IC50 = 24.0 nM 7.62 Invitrogen kinase assay (ZAP70) -
Mast cell IC50 = 38.0 nM 7.42 Human Mast Cell degranulation -
Tyrosine-protein kinase SYK IC50 = 38.0 nM 7.42 Affinity Phenotypic Cellular interaction (Cellular human mast cell degranulation... -
Tyrosine-protein kinase SYK IC50 = 38.0 nM 7.42 Affinity On-target Cellular interaction (Cellular human mast cell degranulation ... -
Proto-oncogene tyrosine-protein kinase Src IC50 = 100.0 nM 7.0 Invitrogen kinase assay (SRC) -
Proto-oncogene tyrosine-protein kinase Src IC50 = 100.0 nM 7.0 Selectivity interaction (KinomeScan (Invitrogen)) EUB0000714a SRC -
High affinity nerve growth factor receptor IC50 = 105.0 nM 6.98 Invitrogen kinase assay (NTRK1) -
High affinity nerve growth factor receptor IC50 = 105.0 nM 6.98 Selectivity interaction (KinomeScan (Invitrogen)) EUB0000714a NTRK1 -
NT-3 growth factor receptor IC50 = 120.0 nM 6.92 Selectivity interaction (KinomeScan (Invitrogen)) EUB0000714a NTRK3 -
NT-3 growth factor receptor IC50 = 120.0 nM 6.92 Invitrogen kinase assay (NTRK3) -
Tyrosine-protein kinase Fgr IC50 = 185.0 nM 6.73 Invitrogen kinase assay (FGR) -
Tyrosine-protein kinase Fyn IC50 = 205.0 nM 6.69 Invitrogen kinase assay (FYN) -
Tyrosine-protein kinase Fer IC50 = 232.0 nM 6.63 Invitrogen kinase assay (FER) -
Tyrosine-protein kinase JAK2 IC50 = 242.0 nM 6.62 Invitrogen kinase assay (JAK2) -
Cysteinyl leukotriene receptor IC50 = 287.0 nM 6.54 Human Whole Blood Cys LT a-IgE -
Sodium-dependent noradrenaline transporter Ki = 7713.0 nM 5.11 GPCRScan assay: inhibition of NET -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4507285 Tyrosine-protein kinase ABL1 15
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL4507285 Epidermal growth factor receptor 12
- 10.6019/CHEMBL4507285 Receptor-type tyrosine-protein kinase FLT3 11
- 10.6019/CHEMBL4689842 U2OS 10
- 10.6019/CHEMBL4507285 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL4689842 Fibroblast 9
- 10.6019/CHEMBL4507285 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4689842 HEK-293T 8
- 10.6019/CHEMBL5724696 U2OS 8
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4507285 Proto-oncogene tyrosine-protein kinase receptor Ret 4
- 10.6019/CHEMBL4507285 ALK tyrosine kinase receptor 3
- 10.6019/CHEMBL4507285 Hepatocyte growth factor receptor 3
- 10.6019/CHEMBL4507285 Histamine H3 receptor 3
- 10.6019/CHEMBL4507285 Sodium-dependent noradrenaline transporter 3
- 10.6019/CHEMBL4507285 Tyrosine-protein kinase SYK 3
- 10.6019/CHEMBL4507285 Tyrosine-protein kinase ZAP-70 2

Data from ChEMBL 36 via Core Engine