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

CHEMBL5075200

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
COc1ccc(S(=O)(=O)NCCNc2nccc(-c3c(-c4ccccc4)nc4sccn34)n2)cc1

Basic Information

ChEMBL ID CHEMBL5075200
Phase Preclinical
Structure Type MOL
InChI Key DUAGJVFSWKNHNE-UHFFFAOYSA-N
22
Targets
27
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

506.6
MW (Da)
3.92
ALogP
9
HBA
2
HBD
110.5
PSA (Ų)
0.29
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22N6O3S2
MW 506.61
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.85

Activity Summary

IC50 27 meas. best 7.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase B-raf
CHEMBL5145
IC50 7.11 6.725 77.0 6
RAF proto-oncogene serine/threonine-protein kinase
CHEMBL1906
IC50 6.76 6.76 172.0 1
UACC-62
CHEMBL614610
IC50 5.96 5.96 1100.0 1
MDA-MB-435
CHEMBL614697
IC50 5.92 5.92 1200.0 1
SK-MEL-5
CHEMBL614922
IC50 5.77 5.77 1700.0 1
Panel colon (Carcinoma cell lines)
CHEMBL614467
IC50 5.66 5.66 2190.0 1
Panel prostate (Carcinoma cell lines)
CHEMBL614692
IC50 5.61 5.61 2450.0 1
M14
CHEMBL614317
IC50 5.57 5.57 2700.0 1
Panel leukemia (Carcinoma cell lines)
CHEMBL614083
IC50 5.52 5.52 2990.0 1
Panel ovarian (Carcinoma cell lines)
CHEMBL615007
IC50 5.45 5.45 3570.0 1
Panel renal (Carcinoma cell lines)
CHEMBL612516
IC50 5.43 5.43 3700.0 1
LOX IMVI
CHEMBL614096
IC50 5.41 5.41 3900.0 1
Panel melanoma (Carcinoma cell lines)
CHEMBL612280
IC50 5.39 5.39 4030.0 1
SK-MEL-2
CHEMBL614917
IC50 5.31 5.31 4900.0 1
NSCLC
CHEMBL612554
IC50 5.27 5.27 5420.0 1
SK-MEL-28
CHEMBL614919
IC50 5.24 5.24 5700.0 1
Panel CNS (Carcinoma cell lines)
CHEMBL614459
IC50 5.19 5.19 6460.0 1
UACC-257
CHEMBL612796
IC50 5.19 5.19 6400.0 1
Malme-3M
CHEMBL614021
IC50 5.06 5.06 8700.0 1
Panel breast (Carcinoma cell lines)
CHEMBL614362
IC50 4.88 4.88 13300.0 1
BJ
CHEMBL614358
IC50 4.25 4.25 55640.0 1
L132
CHEMBL613999
IC50 4.22 4.22 60250.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase B-raf IC50 = 77.0 nM 7.11 Enzymatic Activity Assay: Reaction biology kinase hotspot service (http://www.re... -
Serine/threonine-protein kinase B-raf IC50 = 77.0 nM 7.11 Kinase Hotspot Assay: Reaction biology kinase hotspot service (http://www.reacti... -
Serine/threonine-protein kinase B-raf IC50 = 77.5 nM 7.11 Inhibition of human BRAF V600E mutant using myelin basic protein as substrate in... 33999621
RAF proto-oncogene serine/threonine-protein kinase IC50 = 172.0 nM 6.76 Inhibition of human wild type CRAF using myelin basic protein as substrate in pr... 33999621
Serine/threonine-protein kinase B-raf IC50 = 459.0 nM 6.34 Inhibition of human wild type BRAF using myelin basic protein as substrate in pr... 33999621
Serine/threonine-protein kinase B-raf IC50 = 459.0 nM 6.34 Enzymatic Activity Assay: Reaction biology kinase hotspot service (http://www.re... -
Serine/threonine-protein kinase B-raf IC50 = 459.0 nM 6.34 Kinase Hotspot Assay: Reaction biology kinase hotspot service (http://www.reacti... -
UACC-62 IC50 = 1100.0 nM 5.96 Antiproliferative activity against human UACC-62 cells assessed as cell growth i... 33999621
MDA-MB-435 IC50 = 1200.0 nM 5.92 Antiproliferative activity against human MDA-MB-435 cells assessed as cell growt... 33999621
SK-MEL-5 IC50 = 1700.0 nM 5.77 Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth ... 33999621
Panel colon (Carcinoma cell lines) IC50 = 2190.0 nM 5.66 Antiproliferative activity against human Panel colon (Carcinoma cell lines) asse... 33999621
Panel prostate (Carcinoma cell lines) IC50 = 2450.0 nM 5.61 Antiproliferative activity against human Panel prostate (Carcinoma cell lines) a... 33999621
M14 IC50 = 2700.0 nM 5.57 Antiproliferative activity against human M14 cells assessed as cell growth inhib... 33999621
Panel leukemia (Carcinoma cell lines) IC50 = 2990.0 nM 5.52 Antiproliferative activity against human Panel leukemia (Carcinoma cell lines) a... 33999621
Panel ovarian (Carcinoma cell lines) IC50 = 3570.0 nM 5.45 Antiproliferative activity against human Panel ovarian (Carcinoma cell lines) as... 33999621
Panel renal (Carcinoma cell lines) IC50 = 3700.0 nM 5.43 Antiproliferative activity against human Panel renal (Carcinoma cell lines) asse... 33999621
LOX IMVI IC50 = 3900.0 nM 5.41 Antiproliferative activity against human LOX IMVI cells assessed as cell growth ... 33999621
Panel melanoma (Carcinoma cell lines) IC50 = 4030.0 nM 5.39 Antiproliferative activity against human Panel melanoma (Carcinoma cell lines) a... 33999621
SK-MEL-2 IC50 = 4900.0 nM 5.31 Antiproliferative activity against human SK-MEL-2 cells assessed as cell growth ... 33999621
NSCLC IC50 = 5420.0 nM 5.27 Antiproliferative activity against human NSCLC cell line assessed as cell growth... 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 Panel leukemia (Carcinoma cell lines) 2
33999621 10.1021/acs.jmedchem.1c00230 Panel colon (Carcinoma cell lines) 2
33999621 10.1021/acs.jmedchem.1c00230 Panel melanoma (Carcinoma cell lines) 2
33999621 10.1021/acs.jmedchem.1c00230 Panel ovarian (Carcinoma cell lines) 2
33999621 10.1021/acs.jmedchem.1c00230 UACC-62 2
33999621 10.1021/acs.jmedchem.1c00230 UACC-257 2
33999621 10.1021/acs.jmedchem.1c00230 SK-MEL-5 2
33999621 10.1021/acs.jmedchem.1c00230 SK-MEL-28 2
33999621 10.1021/acs.jmedchem.1c00230 LOX IMVI 2
33999621 10.1021/acs.jmedchem.1c00230 Malme-3M 2
33999621 10.1021/acs.jmedchem.1c00230 M14 2
33999621 10.1021/acs.jmedchem.1c00230 MDA-MB-435 2
33999621 10.1021/acs.jmedchem.1c00230 SK-MEL-2 2
33999621 10.1021/acs.jmedchem.1c00230 ADMET 1
33999621 10.1021/acs.jmedchem.1c00230 Panel breast (Carcinoma cell lines) 1
33999621 10.1021/acs.jmedchem.1c00230 Panel prostate (Carcinoma cell lines) 1
33999621 10.1021/acs.jmedchem.1c00230 Panel renal (Carcinoma cell lines) 1
33999621 10.1021/acs.jmedchem.1c00230 Panel CNS (Carcinoma cell lines) 1

Data from ChEMBL 36 via Core Engine