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Compound Detail

CHEMBL4537673

BAY-985
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C[C@H](c1ccnc(Nc2nc3ccc(-c4cc(N(C)C)ncn4)cc3[nH]2)c1)N1CCN(C(=O)CC(F)(F)F)CC1

Basic Information

ChEMBL ID CHEMBL4537673
Name BAY-985
Phase Preclinical
Structure Type MOL
InChI Key HZRJHVDNTDBTOZ-QGZVFWFLSA-N
16
Targets
38
Activities
3
Assay Types
6
PK Parameters
20
Publications
0
Known Names

Molecular Properties

553.6
MW (Da)
4.38
ALogP
8
HBA
2
HBD
106.2
PSA (Ų)
0.35
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C27H30F3N9O
MW 553.59
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.46

Activity Summary

IC50 30 meas. best 8.7
Ki 6 meas. best 5.95
Kd 2 meas. best 8.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase TBK1
CHEMBL5408
IC50 8.7 7.69 2.0 8
Inhibitor of nuclear factor kappa-B kinase subunit epsilon
CHEMBL3529
IC50 8.7 7.4583 2.0 6
Mitogen-activated protein kinase kinase kinase 19
CHEMBL6191
Kd 8.02 8.02 9.6 1
IKK epsilon/TBK1
CHEMBL3038486
IC50 7.13 7.13 74.0 1
Serine/threonine-protein kinase 17A
CHEMBL4525
Kd 7.13 7.13 74.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 6.91 6.91 123.0 2
Ribosomal protein S6 kinase alpha-6
CHEMBL4924
IC50 6.56 6.56 276.0 2
Serine/threonine-protein kinase 17A
CHEMBL4525
IC50 6.51 6.51 310.0 3
Cytochrome P450 2C8
CHEMBL3721
IC50 6.07 6.07 860.0 1
Dual specificity mitogen-activated protein kinase kinase 5
CHEMBL4948
IC50 6.07 6.07 847.0 1
SK-MEL-2
CHEMBL614917
IC50 6.05 6.05 900.0 1
Sigma intracellular receptor 2
CHEMBL4105907
Ki 5.95 5.9433 1122.0 3
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 5.89 5.8833 1288.2 3
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.33 5.33 4700.0 1
ACHN
CHEMBL614519
IC50 5.14 5.14 7260.0 1
Serine/threonine-protein kinase ULK1
CHEMBL6006
IC50 5.1 5.1 7930.0 2
Cytochrome P450 2C9
CHEMBL3397
IC50 4.77 4.77 17000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 8.333 mL.min-1.kg-1 Homo sapiens
CL 28.33 mL.min-1.kg-1 Rattus norvegicus
CL 28.33 mL.min-1.kg-1 Rattus norvegicus
CL 66.67 mL.min-1.kg-1 Rattus norvegicus
F 11.0 % Rattus norvegicus
T1/2 0.79 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Inhibitor of nuclear factor kappa-B kinase subunit epsilon IC50 = 2.0 nM 8.7 Inhibition of recombinant full length human C-terminal GST-tagged IKKepsilon exp... 31859507
Serine/threonine-protein kinase TBK1 IC50 = 2.0 nM 8.7 Inhibition of recombinant full length human N-terminal His-tagged TBK1 using bio... 31859507
Inhibitor of nuclear factor kappa-B kinase subunit epsilon IC50 = 2.0 nM 8.7 Affinity Biochemical interaction (TR-FRET-based kinase activity inhibition assay... -
Serine/threonine-protein kinase TBK1 IC50 = 2.0 nM 8.7 Affinity Biochemical interaction (TR-FRET-based kinase activity inhibition assay... -
Inhibitor of nuclear factor kappa-B kinase subunit epsilon IC50 = 2.0 nM 8.7 Biochemical assay (low ATP) with IKBKE -
Serine/threonine-protein kinase TBK1 IC50 = 2.0 nM 8.7 Biochemical assay (low ATP) with TBK1 -
Mitogen-activated protein kinase kinase kinase 19 Kd = 9.6 nM 8.02 Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0... -
Serine/threonine-protein kinase TBK1 IC50 = 18.0 nM 7.75 Biochemical assay (high ATP) with TBK1 -
Serine/threonine-protein kinase TBK1 IC50 = 30.0 nM 7.52 Inhibition of recombinant full length human N-terminal His-tagged TBK1 using bio... 31859507
IKK epsilon/TBK1 IC50 = 74.0 nM 7.13 Inhibition of IKKepsilon/TBK1 in human MDB-MB-231 cells transduced with lentivir... 31859507
Serine/threonine-protein kinase TBK1 IC50 = 74.0 nM 7.13 Affinity Phenotypic Cellular interaction (pIRF3 cell-based mechanistic assay in ... -
Inhibitor of nuclear factor kappa-B kinase subunit epsilon IC50 = 74.0 nM 7.13 Affinity Phenotypic Cellular interaction (pIRF3 cell-based mechanistic assay in ... -
Serine/threonine-protein kinase 17A Kd = 74.0 nM 7.13 Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0... -
Receptor-type tyrosine-protein kinase FLT3 IC50 = 123.0 nM 6.91 Inhibition of recombinant human N-terminal GST-tagged FLT3 (564 to end residues)... 31859507
Receptor-type tyrosine-protein kinase FLT3 IC50 = 123.0 nM 6.91 Selectivity interaction (Enzymatic assay) EUB0000305b FLT3 -
Ribosomal protein S6 kinase alpha-6 IC50 = 276.0 nM 6.56 Inhibition of recombinant full length human His6-tagged RSK4 expressed in baculo... 31859507
Ribosomal protein S6 kinase alpha-6 IC50 = 276.0 nM 6.56 Selectivity interaction (Enzymatic assay) EUB0000305b RPS6KA6 -
Serine/threonine-protein kinase 17A IC50 = 310.0 nM 6.51 Selectivity interaction (Enzymatic assay (Eurofins)) EUB0000305b STK17A -
Serine/threonine-protein kinase TBK1 IC50 = 312.0 nM 6.51 Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000... -
Serine/threonine-protein kinase 17A IC50 = 311.0 nM 6.51 Selectivity interaction (Enzymatic assay) EUB0000305b STK17A -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4507318 Tyrosine-protein kinase ABL1 15
31859507 10.1021/acs.jmedchem.9b01460 ADMET 15
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL4507318 Epidermal growth factor receptor 12
- 10.6019/CHEMBL4507318 Receptor-type tyrosine-protein kinase FLT3 12
- 10.6019/CHEMBL4689842 Fibroblast 10
- 10.6019/CHEMBL4507318 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL4689842 U2OS 10
- 10.6019/CHEMBL4507318 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4507318 Unchecked 8
- 10.6019/CHEMBL5303304 HEK-293T 7
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.6019/CHEMBL5303304 Fibroblast 5
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL5212743 Serine/threonine-protein kinase 17A 5
31859507 10.1021/acs.jmedchem.9b01460 Unchecked 4
- 10.6019/CHEMBL4507318 Proto-oncogene tyrosine-protein kinase receptor Ret 4
- 10.6019/CHEMBL4507318 Serine/threonine-protein kinase TBK1 4
- 10.6019/CHEMBL4507318 ALK tyrosine kinase receptor 3

Data from ChEMBL 36 via Core Engine