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Compound Detail

CHEMBL4520788

BAY-294
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CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1

Basic Information

ChEMBL ID CHEMBL4520788
Name BAY-294
Phase Preclinical
Structure Type MOL
InChI Key WEGLOYDTDILXDA-HNNXBMFYSA-N
38
Targets
109
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

448.6
MW (Da)
5.58
ALogP
7
HBA
2
HBD
68.3
PSA (Ų)
0.37
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 C25H28N4O2S
MW 448.59
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.75

Activity Summary

Ki 89 meas. best 7.67
IC50 20 meas. best 5.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H2 receptor
CHEMBL1941
Ki 7.67 7.67 21.1 3
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 7.16 7.16 69.2 3
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 7.13 7.13 74.1 3
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.07 7.0367 86.1 3
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 7.04 7.0267 91.2 3
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 7.04 7.0333 92.3 3
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.9 6.8933 125.9 3
Muscarinic acetylcholine receptor M1
CHEMBL216
Ki 6.65 6.4533 223.9 3
Muscarinic acetylcholine receptor M4
CHEMBL1821
Ki 6.54 6.5267 291.7 3
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.41 6.4033 389.1 3
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.41 6.41 389.1 3
Alpha-1A adrenergic receptor
CHEMBL229
Ki 6.36 6.35 436.5 2
Muscarinic acetylcholine receptor M5
CHEMBL2035
Ki 6.28 6.28 523.9 3
D(1A) dopamine receptor
CHEMBL2056
Ki 6.25 6.1767 562.3 3
Sigma intracellular receptor 2
CHEMBL4105907
Ki 6.21 6.2033 609.5 3
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 6.16 6.16 691.8 3
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.16 6.1533 691.8 3
Mu-type opioid receptor
CHEMBL233
Ki 6.12 6.0867 758.6 3
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 6.09 6.0767 812.8 3
Kappa-type opioid receptor
CHEMBL237
Ki 6.08 6.08 822.2 3
D(3) dopamine receptor
CHEMBL234
Ki 6.06 6.06 868.6 3
5-hydroxytryptamine receptor 5A
CHEMBL3426
Ki 6.01 5.99 977.2 3
Histamine H1 receptor
CHEMBL231
Ki 5.87 5.87 1349.0 3
Sodium-dependent dopamine transporter
CHEMBL238
Ki 5.85 5.8033 1412.5 3
Muscarinic acetylcholine receptor M2
CHEMBL211
Ki 5.83 5.83 1474.0 3
5-hydroxytryptamine receptor 1B
CHEMBL1898
Ki 5.76 5.7533 1737.8 3
Calu-1
CHEMBL613505
IC50 5.74 5.74 1840.0 1
Histamine H4 receptor
CHEMBL3759
Ki 5.72 5.72 1885.8 3
Son of sevenless homolog 1
CHEMBL2079846
IC50 5.72 5.3967 1890.0 9
D(2) dopamine receptor
CHEMBL217
Ki 5.7 5.6533 1995.3 3
Sodium-dependent noradrenaline transporter
CHEMBL222
Ki 5.68 5.68 2083.2 3
SOS1-KRAS
CHEMBL5465393
IC50 5.63 5.63 2340.0 4
NCI-H358
CHEMBL614135
IC50 5.47 5.47 3390.0 1
RAS
CHEMBL4524006
IC50 5.38 5.055 4120.0 2
Sodium-dependent serotonin transporter
CHEMBL228
Ki 5.37 5.37 4231.6 3
Mitogen-activated protein kinase 1
CHEMBL4040
IC50 5.34 5.34 4570.0 1
K562
CHEMBL385
IC50 5.12 5.12 7500.0 1
MOLM-13
CHEMBL3706572
IC50 5.12 5.12 7570.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H2 receptor Ki = 21.13 nM 7.67 GPCRScan assay: inhibition of H2 -
Histamine H2 receptor Ki = 21.13 nM 7.67 GPCRScan assay: inhibition of H2 -
Histamine H2 receptor Ki = 21.13 nM 7.67 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH2 -
5-hydroxytryptamine receptor 2A Ki = 69.37 nM 7.16 GPCRScan assay: inhibition of 5-HT2A -
5-hydroxytryptamine receptor 2A Ki = 69.18 nM 7.16 GPCRScan assay: inhibition of 5-HT2A -
5-hydroxytryptamine receptor 2A Ki = 69.37 nM 7.16 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR2A -
5-hydroxytryptamine receptor 2B Ki = 74.56 nM 7.13 GPCRScan assay: inhibition of 5-HT2B -
5-hydroxytryptamine receptor 2B Ki = 74.13 nM 7.13 GPCRScan assay: inhibition of 5-HT2B -
5-hydroxytryptamine receptor 2B Ki = 74.56 nM 7.13 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR2B -
Alpha-1B adrenergic receptor Ki = 86.1 nM 7.07 GPCRScan assay: inhibition of Alpha1B -
5-hydroxytryptamine receptor 1D Ki = 92.26 nM 7.04 GPCRScan assay: inhibition of 5-HT1D -
Alpha-2C adrenergic receptor Ki = 91.2 nM 7.04 GPCRScan assay: inhibition of Alpha2C -
5-hydroxytryptamine receptor 1D Ki = 93.49 nM 7.03 GPCRScan assay: inhibition of 5-HT1D -
5-hydroxytryptamine receptor 1D Ki = 93.49 nM 7.03 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR1D -
Alpha-2C adrenergic receptor Ki = 95.18 nM 7.02 GPCRScan assay: inhibition of Alpha2C -
Alpha-2C adrenergic receptor Ki = 95.18 nM 7.02 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a ADRA2C -
Alpha-1B adrenergic receptor Ki = 95.26 nM 7.02 Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a ADRA1B -
Alpha-1B adrenergic receptor Ki = 95.26 nM 7.02 GPCRScan assay: inhibition of Alpha1B -
Alpha-2A adrenergic receptor Ki = 125.89 nM 6.9 GPCRScan assay: inhibition of Alpha2A -
Alpha-2A adrenergic receptor Ki = 127.42 nM 6.89 GPCRScan assay: inhibition of Alpha2A -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4689842 U2OS 429
- 10.6019/CHEMBL4689842 HEK-293T 428
- 10.6019/CHEMBL4689842 Fibroblast 428
- 10.6019/CHEMBL4507273 Tyrosine-protein kinase ABL1 15
- 10.6019/CHEMBL4507273 Epidermal growth factor receptor 13
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL4507273 Receptor-type tyrosine-protein kinase FLT3 11
30683722 10.1073/pnas.1812963116 Son of sevenless homolog 1 10
- 10.6019/CHEMBL4507273 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL4507273 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4507273 Unchecked 8
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4507273 Proto-oncogene tyrosine-protein kinase receptor Ret 4
- 10.6019/CHEMBL4507273 5-hydroxytryptamine receptor 1A 3
- 10.6019/CHEMBL4507273 Muscarinic acetylcholine receptor M2 3
- 10.6019/CHEMBL4507273 5-hydroxytryptamine receptor 1D 3
- 10.6019/CHEMBL4507273 Sodium-dependent serotonin transporter 3
- 10.6019/CHEMBL4507273 Hepatocyte growth factor receptor 3

Data from ChEMBL 36 via Core Engine