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

CHEMBL5083036

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
O=S(=O)(NCCNc1nccc(-c2c(-c3cccc(O)c3)nc3sccn23)n1)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL5083036
Phase Preclinical
Structure Type MOL
InChI Key YDYJBUHNTGURQT-UHFFFAOYSA-N
32
Targets
37
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

510.6
MW (Da)
3.75
ALogP
9
HBA
3
HBD
121.5
PSA (Ų)
0.27
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H19FN6O3S2
MW 510.58
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.90

Activity Summary

IC50 37 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase B-raf
CHEMBL5145
IC50 9.0 8.675 1.0 6
RAF proto-oncogene serine/threonine-protein kinase
CHEMBL1906
IC50 8.22 8.22 6.0 1
UACC-62
CHEMBL614610
IC50 6.57 6.57 270.0 1
Malme-3M
CHEMBL614021
IC50 6.55 6.55 279.0 1
M14
CHEMBL614317
IC50 6.25 6.25 567.0 1
UACC-257
CHEMBL612796
IC50 6.25 6.25 568.0 1
SK-MEL-28
CHEMBL614919
IC50 6.18 6.18 660.0 1
MDA-MB-435
CHEMBL614697
IC50 6.03 6.03 939.0 1
Mitogen-activated protein kinase 11
CHEMBL3961
IC50 5.92 5.92 1210.0 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.87 5.87 1350.0 1
Panel melanoma (Carcinoma cell lines)
CHEMBL612280
IC50 5.83 5.83 1490.0 1
SK-MEL-5
CHEMBL614922
IC50 5.79 5.79 1610.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 5.7 5.7 1990.0 1
Mitogen-activated protein kinase 14
CHEMBL260
IC50 5.7 5.7 2010.0 1
Panel leukemia (Carcinoma cell lines)
CHEMBL614083
IC50 5.55 5.55 2820.0 1
NSCLC
CHEMBL612554
IC50 5.49 5.49 3260.0 1
LOX IMVI
CHEMBL614096
IC50 5.39 5.39 4110.0 1
Panel breast (Carcinoma cell lines)
CHEMBL614362
IC50 5.39 5.39 4100.0 1
SK-MEL-2
CHEMBL614917
IC50 5.35 5.35 4490.0 1
Homeodomain-interacting protein kinase 1
CHEMBL5427
IC50 5.29 5.29 5130.0 1
Panel renal (Carcinoma cell lines)
CHEMBL612516
IC50 5.27 5.27 5380.0 1
Panel colon (Carcinoma cell lines)
CHEMBL614467
IC50 5.27 5.27 5420.0 1
Panel prostate (Carcinoma cell lines)
CHEMBL614692
IC50 5.14 5.14 7300.0 1
Mitogen-activated protein kinase kinase kinase 20
CHEMBL3886
IC50 5.12 5.12 7580.0 1
Panel CNS (Carcinoma cell lines)
CHEMBL614459
IC50 5.12 5.12 7580.0 1
BDNF/NT-3 growth factors receptor
CHEMBL4898
IC50 5.06 5.06 8710.0 1
Serine/threonine-protein kinase/endoribonuclease IRE1
CHEMBL1163101
IC50 5.02 5.02 9540.0 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 5.02 5.02 9580.0 1
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 4.98 4.98 10370.0 1
Panel ovarian (Carcinoma cell lines)
CHEMBL615007
IC50 4.85 4.85 14180.0 1
BJ
CHEMBL614358
IC50 4.3 4.3 50620.0 1
L132
CHEMBL613999
IC50 4.28 4.28 52370.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase B-raf IC50 = 1.0 nM 9.0 Enzymatic Activity Assay: Reaction biology kinase hotspot service (http://www.re... -
Serine/threonine-protein kinase B-raf IC50 = 1.0 nM 9.0 Inhibition of human BRAF V600E mutant using myelin basic protein as substrate in... 33999621
Serine/threonine-protein kinase B-raf IC50 = 1.0 nM 9.0 Kinase Hotspot Assay: Reaction biology kinase hotspot service (http://www.reacti... -
Serine/threonine-protein kinase B-raf IC50 = 2.7 nM 8.57 Inhibition of human wild type BRAF using myelin basic protein as substrate in pr... 33999621
Serine/threonine-protein kinase B-raf IC50 = 5.7 nM 8.24 Enzymatic Activity Assay: Reaction biology kinase hotspot service (http://www.re... -
Serine/threonine-protein kinase B-raf IC50 = 5.7 nM 8.24 Kinase Hotspot Assay: Reaction biology kinase hotspot service (http://www.reacti... -
RAF proto-oncogene serine/threonine-protein kinase IC50 = 6.0 nM 8.22 Inhibition of human wild type CRAF using myelin basic protein as substrate in pr... 33999621
UACC-62 IC50 = 270.0 nM 6.57 Antiproliferative activity against human UACC-62 cells assessed as cell growth i... 33999621
Malme-3M IC50 = 279.0 nM 6.55 Antiproliferative activity against human Malme-3M cells assessed as cell growth ... 33999621
M14 IC50 = 567.0 nM 6.25 Antiproliferative activity against human M14 cells assessed as cell growth inhib... 33999621
UACC-257 IC50 = 568.0 nM 6.25 Antiproliferative activity against human UACC-257 cells assessed as cell growth ... 33999621
SK-MEL-28 IC50 = 660.0 nM 6.18 Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth... 33999621
MDA-MB-435 IC50 = 939.0 nM 6.03 Antiproliferative activity against human MDA-MB-435 cells assessed as cell growt... 33999621
Mitogen-activated protein kinase 11 IC50 = 1210.0 nM 5.92 Inhibition of MAPK11 (unknown origin) incubated for 1 hr by qPCR analysis 33999621
Mitogen-activated protein kinase 8 IC50 = 1350.0 nM 5.87 Inhibition of MAPK8 (unknown origin) incubated for 1 hr by qPCR analysis 33999621
Panel melanoma (Carcinoma cell lines) IC50 = 1490.0 nM 5.83 Antiproliferative activity against human Panel melanoma (Carcinoma cell lines) a... 33999621
SK-MEL-5 IC50 = 1610.0 nM 5.79 Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth ... 33999621
Mitogen-activated protein kinase 14 IC50 = 2010.0 nM 5.7 Inhibition of MAPK14 (unknown origin) incubated for 1 hr by qPCR analysis 33999621
Receptor-type tyrosine-protein kinase FLT3 IC50 = 1990.0 nM 5.7 Inhibition of FLT3 (unknown origin) incubated for 1 hr by qPCR analysis 33999621
Panel leukemia (Carcinoma cell lines) IC50 = 2820.0 nM 5.55 Antiproliferative activity against human Panel leukemia (Carcinoma cell lines) a... 33999621

Literature References

PubMed DOI Target Context # Activities
33999621 10.1021/acs.jmedchem.1c00230 Serine/threonine-protein kinase B-raf 4
33999621 10.1021/acs.jmedchem.1c00230 RAF proto-oncogene serine/threonine-protein kinase 2
33999621 10.1021/acs.jmedchem.1c00230 LOX IMVI 2
33999621 10.1021/acs.jmedchem.1c00230 M14 2
33999621 10.1021/acs.jmedchem.1c00230 Unchecked 2
33999621 10.1021/acs.jmedchem.1c00230 MDA-MB-435 2
33999621 10.1021/acs.jmedchem.1c00230 SK-MEL-5 2
33999621 10.1021/acs.jmedchem.1c00230 UACC-62 2
33999621 10.1021/acs.jmedchem.1c00230 Panel melanoma (Carcinoma cell lines) 2
33999621 10.1021/acs.jmedchem.1c00230 SK-MEL-2 2
33999621 10.1021/acs.jmedchem.1c00230 SK-MEL-28 2
33999621 10.1021/acs.jmedchem.1c00230 UACC-257 2
33999621 10.1021/acs.jmedchem.1c00230 Mitogen-activated protein kinase kinase kinase 20 1
33999621 10.1021/acs.jmedchem.1c00230 BDNF/NT-3 growth factors receptor 1
33999621 10.1021/acs.jmedchem.1c00230 Mitogen-activated protein kinase 11 1
33999621 10.1021/acs.jmedchem.1c00230 Panel leukemia (Carcinoma cell lines) 1
33999621 10.1021/acs.jmedchem.1c00230 Mitogen-activated protein kinase 8 1
33999621 10.1021/acs.jmedchem.1c00230 Receptor-type tyrosine-protein kinase FLT3 1
33999621 10.1021/acs.jmedchem.1c00230 ADMET 1
33999621 10.1021/acs.jmedchem.1c00230 Fibroblast growth factor receptor 1 1

Data from ChEMBL 36 via Core Engine