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Compound Detail

CHEMBL1240885

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Nc1ncnc2[nH]nc(Nc3ccc(F)cc3)c12

Basic Information

ChEMBL ID CHEMBL1240885
Phase Preclinical
Structure Type MOL
InChI Key UQPMANVRZYYQMD-UHFFFAOYSA-N
13
Targets
40
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

244.2
MW (Da)
1.82
ALogP
5
HBA
3
HBD
92.5
PSA (Ų)
0.64
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H9FN6
MW 244.23
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -1.45

Activity Summary

IC50 36 meas. best 6.29
Ki 4 meas. best 6.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
Ki 6.47 6.265 340.0 2
Casein kinase I isoform delta
CHEMBL2828
IC50 6.29 6.29 510.0 1
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
IC50 6.2 5.9838 628.2 13
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
Ki 6.0 6.0 1010.0 2
Serine/threonine-protein kinase BRSK2
CHEMBL4574
IC50 5.96 5.96 1100.0 1
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
IC50 5.82 5.7473 1530.0 11
Aurora kinase B
CHEMBL2185
IC50 5.6 5.6 2500.0 1
Proto-oncogene tyrosine-protein kinase LCK
CHEMBL2480
IC50 5.6 5.6 2500.0 1
Serine/threonine-protein kinase Sgk1
CHEMBL2343
IC50 5.57 5.57 2700.0 2
Eukaryotic translation initiation factor 4E
CHEMBL4848
IC50 5.52 5.52 3000.0 1
Dual specificity tyrosine-phosphorylation-regulated kinase 3
CHEMBL4575
IC50 5.5 5.5 3200.0 1
Interferon-induced, double-stranded RNA-activated protein kinase
CHEMBL5785
IC50 5.3 5.3 5000.0 1
MOLM-13
CHEMBL3706572
IC50 5.08 5.08 8240.0 1
HCT-116
CHEMBL394
IC50 4.99 4.99 10210.0 1
THP-1
CHEMBL614245
IC50 4.93 4.93 11680.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MAP kinase-interacting serine/threonine-protein kinase 2 Ki = 340.0 nM 6.47 Inhibition of human Mnk2a using TAMRA-labeled eIF4E peptide as substrate incubat... 26408454
Casein kinase I isoform delta IC50 = 510.0 nM 6.29 Inhibition of CK1delta in the presence of 20uM ATP 17850214
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 628.2 nM 6.2 Inhibition of Mnk1 (unknown origin) incubated for 60 mins in presence of ATP/sub... 38759457
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 850.0 nM 6.07 Inhibition of MNK1 (unknown origin) using S3 as substrate measured after 60 mins... 30115493
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 870.0 nM 6.06 Inhibition of MNK1 in the presence of 50uM ATP 17850214
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 870.0 nM 6.06 Inhibition of MNK1 20722422
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 870.0 nM 6.06 Inhibition of Mnk1a (unknown origin) using TAMRA-labeled eIF4E peptide as substr... 26408454
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 870.0 nM 6.06 Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrea... 30530193
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 870.0 nM 6.06 Inhibition of MKN1 (unknown origin) in presence of ATP by HTRF assay 34515481
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 870.0 nM 6.06 Inhibition of MNK1 (unknown origin) using eIF4E as a substrate in presence of AT... 33892273
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 870.0 nM 6.06 Inhibition of human His6-tagged Mnk1 expressed in Escherichia coli assessed as p... 34533957
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 870.0 nM 6.06 Inhibition of Mnk1 (unknown origin) 38759457
MAP kinase-interacting serine/threonine-protein kinase 2 Ki = 880.0 nM 6.06 Inhibition of Mnk2 (unknown origin) pre-incubated for 10 mins before eIF4E pepti... 25800647
MAP kinase-interacting serine/threonine-protein kinase 1 Ki = 1010.0 nM 6.0 Inhibition of Mnk1a (unknown origin) using TAMRA-labeled eIF4E peptide as substr... 26408454
MAP kinase-interacting serine/threonine-protein kinase 1 Ki = 1010.0 nM 6.0 Inhibition of Mnk1 (unknown origin) pre-incubated for 10 mins before eIF4E pepti... 25800647
Serine/threonine-protein kinase BRSK2 IC50 = 1100.0 nM 5.96 Inhibition of BRSK2 in the presence of 50uM ATP 17850214
MAP kinase-interacting serine/threonine-protein kinase 2 IC50 = 1530.0 nM 5.82 Inhibition of MNK2 (unknown origin) using S3 as substrate measured after 60 mins... 30115493
MAP kinase-interacting serine/threonine-protein kinase 1 IC50 = 1520.0 nM 5.82 Inhibition of human recombinant full length GST-tagged MNK1 expressed in baculov... 35417652
MAP kinase-interacting serine/threonine-protein kinase 2 IC50 = 1600.0 nM 5.8 Inhibition of human Mnk2a using TAMRA-labeled eIF4E peptide as substrate incubat... 26408454
MAP kinase-interacting serine/threonine-protein kinase 2 IC50 = 1600.0 nM 5.8 Inhibition of MNK2 in the presence of 50uM ATP 17850214

Literature References

PubMed DOI Target Context # Activities
25800647 10.1016/j.ejmech.2015.03.032 MV4-11 14
34515481 10.1021/acs.jmedchem.1c01084 MOLM-13 13
23398362 10.1042/bj20121418 Tyrosine-protein kinase Lck 4
23398362 10.1042/bj20121418 Insulin receptor 4
23398362 10.1042/bj20121418 cGMP-dependent protein kinase 1 4
38759457 10.1016/j.ejmech.2024.116499 K562 4
23398362 10.1042/bj20121418 Insulin-like growth factor 1 receptor 4
23398362 10.1042/bj20121418 Serine/threonine-protein kinase mTOR 4
23398362 10.1042/bj20121418 Protein kinase C beta type 4
23398362 10.1042/bj20121418 Tyrosine-protein kinase HCK 4
23398362 10.1042/bj20121418 Cyclin-dependent kinase 5/CDK5 activator 1 4
38759457 10.1016/j.ejmech.2024.116499 MOLM-13 4
26408454 10.1016/j.ejmech.2015.09.008 MAP kinase-interacting serine/threonine-protein kinase 2 3
34515481 10.1021/acs.jmedchem.1c01084 Unchecked 3
23398362 10.1042/bj20121418 Casein kinase I isoform gamma-3 2
23398362 10.1042/bj20121418 Cyclin-dependent kinase 2/cyclin A 2
23398362 10.1042/bj20121418 Fibroblast growth factor receptor 3 2
23398362 10.1042/bj20121418 Tyrosine-protein kinase ABL2 2
23398362 10.1042/bj20121418 Ephrin type-A receptor 4 2
23398362 10.1042/bj20121418 Calcium/calmodulin-dependent protein kinase type 1D 2

Data from ChEMBL 36 via Core Engine