Compile Data Set for Download or QSAR
Report error Found 913 of affinity data for UniProtKB/TrEMBL: Q5R2V5
TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 47438BDBM47438(US20240124450, Example 19B)
Affinity DataIC50: 0.100nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 668206BDBM668206(US20240124450, Example 45)
Affinity DataIC50: 0.100nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 47416BDBM47416(US20240124450, Example 6B)
Affinity DataIC50: 0.100nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 668214BDBM668214(US20240124450, Example 53)
Affinity DataIC50: 0.100nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 668167BDBM668167(US20240124450, Example 18)
Affinity DataIC50: 0.100nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808701BDBM808701(6-(2-chloro-6-methyl-phenyl)-N8-(1- methyl-4-piper...)
Affinity DataKi:  0.176nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808687BDBM808687(N-[7-(2-fluoro-6-methyl-phenyl)-5- [(1-methyl-4-pi...)
Affinity DataKi:  0.183nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808618BDBM808618(7-(2-fluoro-6-methyl-phenyl)-5-(4- piperidyloxy)is...)
Affinity DataKi:  0.192nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 50660685BDBM50660685(CHEMBL6159758)
Affinity DataIC50: 0.193nMAssay Description:Inhibition of human SIK1 (02 to 131) assessed as luminescence signal using AMARAtide/ATP as substrate measured after 120 mins by microplate readerMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
6/5/2026
Entry Details
PubMed
TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 47433BDBM47433(US20240124450, Example 15B)
Affinity DataIC50: 0.200nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 47435BDBM47435(US20240124450, Example 17B)
Affinity DataIC50: 0.200nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 668204BDBM668204(US20240124450, Example 43)
Affinity DataIC50: 0.200nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 668154BDBM668154(US20240124450, Example 11A)
Affinity DataIC50: 0.200nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 47425BDBM47425(US20240124450, Example 11B)
Affinity DataIC50: 0.200nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 668208BDBM668208(US20240124450, Example 47)
Affinity DataIC50: 0.200nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 50660686BDBM50660686(CHEMBL6148877)
Affinity DataIC50: 0.234nMAssay Description:Inhibition of human SIK1 (02 to 131) assessed as luminescence signal using AMARAtide/ATP as substrate measured after 120 mins by microplate readerMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
6/5/2026
Entry Details
PubMed
TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808595BDBM808595(N5-[(3S)-azepan-3-yl]-7-(2-fluoro-6- methyl-phenyl...)
Affinity DataKi:  0.287nMAssay Description:An enzymatic assay with recombinant human CHIT1 was used in order to establish inhibitory activity of the compounds (Boot et al., 2001, JBC: 276). Th...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808709BDBM808709(6-(2-chloro-6-methyl-phenyl)-N8-(4- piperidyl)quin...)
Affinity DataKi:  0.296nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 47424BDBM47424(US20240124450, Example 10B)
Affinity DataIC50: 0.300nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 668197BDBM668197(US20240124450, Example 36 | US20240124450, Example...)
Affinity DataIC50: 0.300nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808641BDBM808641(7-(2-fluoro-6-methyl-phenyl)-N5- [(3R)-1-methylpyr...)
Affinity DataKi:  0.300nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808598BDBM808598(7-(2-fluoro-6-methyl-phenyl)-N5- [(3S)-3-piperidyl...)
Affinity DataKi:  0.302nMAssay Description:An enzymatic assay with recombinant human CHIT1 was used in order to establish inhibitory activity of the compounds (Boot et al., 2001, JBC: 276). Th...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808578BDBM808578(7-(2-fluoro-6-methyl-phenyl)-N5- [[(3R)-pyrrolidin...)
Affinity DataKi:  0.310nMAssay Description:An enzymatic assay with recombinant human AMCase was used in order to establish inhibitory activity of the compounds (Boot et al., 2001, JBC: 276). T...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808581BDBM808581(7-(2-fluoro-6-methyl-phenyl)-N5- [[(3S)-pyrrolidin...)
Affinity DataKi:  0.316nMAssay Description:An enzymatic assay with recombinant human AMCase was used in order to establish inhibitory activity of the compounds (Boot et al., 2001, JBC: 276). T...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808704BDBM808704(6-(2-fluoro-6-methyl-phenyl)-N8-(1- methyl-4-piper...)
Affinity DataKi:  0.317nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808696BDBM808696(6-(2-Fluoro-6-methyl-phenyl)-N8-(4- piperidyl)quin...)
Affinity DataKi:  0.338nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808620BDBM808620(7-(2-fluoro-6-methyl-phenyl)-5-[(3R)- pyrrolidin-3...)
Affinity DataKi:  0.338nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808705BDBM808705(3-amino-7-(2-fluoro-6-methyl- phenyl)-5-(4- piperi...)
Affinity DataKi:  0.348nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808576BDBM808576(7-(2-fluoro-6-methyl-phenyl)-N5- [(3R)-pyrrolidin-...)
Affinity DataKi:  0.354nMAssay Description:The assays were performed in 384-well white opaque plates at 37° C. using the fluorogenic peptide substrates at a concentration of 10 μM in Assa...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808707BDBM808707(6-fluoro-7-(2-fluoro-6-methyl- phenyl)-N5-(1-methy...)
Affinity DataKi:  0.361nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808568BDBM808568(7-(2-fluoro-6-methyl-phenyl)-N5-(4- piperidyl)isoq...)
Affinity DataKi:  0.364nMAssay Description:The assays were performed in 384-well white opaque plates at 37° C. using the fluorogenic peptide substrates at a concentration of 10 μM in Assa...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808601BDBM808601(7-(2-fluoro-6-methyl-phenyl)-5-[3- (methylamino)az...)
Affinity DataKi:  0.381nMAssay Description:The assays were performed in 384-well white opaque plates at 37° C. using the fluorogenic peptide substrates at a concentration of 10 μM in Assa...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 130909BDBM130909(US8822500, Stauro- sporine | US9920060, Staurospor...)
Affinity DataIC50: 0.392nMAssay Description:Inhibition of human SIK1 using AMARAASAAALARRR as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 668201BDBM668201(US20240124450, Example 40)
Affinity DataIC50: 0.400nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 668209BDBM668209(US20240124450, Example 48)
Affinity DataIC50: 0.400nMAssay Description:Salt Induced Kinase (SIK) activity is determined by measuring the effect of a test agent on the activity of the appropriate SIK enzyme to phosphoryla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/9/2024
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 794503BDBM794503(US20260062387, Example 34)
Affinity DataIC50: 0.400nMAssay Description:NIH Molecular Libraries Screening Centers Network [MLSCN] Emory Chemical Biology Discovery Center in MLSCN Assay provider: Dr. Randal Kaufman, Univer...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
7/15/2026
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808656BDBM808656(5-[(3R)-3-(dimethylamino)-1- piperidyl]-7-(2-fluor...)
Affinity DataKi:  0.409nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808700BDBM808700(6-(2-chloro-6-methyl-phenyl)-N8-(1- ethyl-4-piperi...)
Affinity DataKi:  0.409nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808579BDBM808579(7-(2-fluoro-6-methyl-phenyl)-N5- [(3S)-pyrrolidin-...)
Affinity DataKi:  0.414nMAssay Description:An enzymatic assay with recombinant human AMCase was used in order to establish inhibitory activity of the compounds (Boot et al., 2001, JBC: 276). T...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808583BDBM808583(N5-(azetidin-3-ylmethyl)-7-(2-fluoro- 6-methyl-phe...)
Affinity DataKi:  0.417nMAssay Description:An enzymatic assay with recombinant human AMCase was used in order to establish inhibitory activity of the compounds (Boot et al., 2001, JBC: 276). T...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808626BDBM808626(7-(2-fluoro-6-methyl-phenyl)-N5-(1- methyl-4-piper...)
Affinity DataKi:  0.418nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808599BDBM808599(7-(2-fluoro-6-methyl-phenyl)-N3- methyl-N5-(4-pipe...)
Affinity DataKi:  0.429nMAssay Description:The assays were performed in 384-well white opaque plates at 37° C. using the fluorogenic peptide substrates at a concentration of 10 μM in Assa...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808650BDBM808650(7-(2-fluoro-6-methyl-phenyl)-N5- [[(2S)-1-methyl-2...)
Affinity DataKi:  0.433nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808642BDBM808642(7-(2-fluoro-6-methyl-phenyl)-N5- [(3S)-1-methylpyr...)
Affinity DataKi:  0.439nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 2579BDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 0.458nMAssay Description:Inhibition of human SIK1 using AMARAASAAALARRR as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808646BDBM808646(7-(2-fluoro-6-methyl-phenyl)-N5- [[(3S)-1-methylpy...)
Affinity DataKi:  0.461nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808589BDBM808589(N5-[(3R)-azepan-3-yl]-7-(2-fluoro-6- methyl-phenyl...)
Affinity DataKi:  0.463nMAssay Description:An enzymatic assay with recombinant human AMCase was used in order to establish inhibitory activity of the compounds (Boot et al., 2001, JBC: 276). T...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808602BDBM808602(7-(2-chloro-6-methyl-phenyl)-N5-(4- piperidyl)isoq...)
Affinity DataKi:  0.474nMAssay Description:The assays were performed in 384-well white opaque plates at 37° C. using the fluorogenic peptide substrates at a concentration of 10 μM in Assa...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808591BDBM808591(7-(2-fluoro-6-methyl-phenyl)-5-[(3R)- 3-(methylami...)
Affinity DataKi:  0.476nMAssay Description:An enzymatic assay with recombinant human AMCase was used in order to establish inhibitory activity of the compounds (Boot et al., 2001, JBC: 276). T...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase SIK1(Human)
Pfizer

US Patent
LigandChemical structure of BindingDB Monomer ID 808634BDBM808634(7-(2-chloro-6-methyl-phenyl)-N5-(1- methyl-4-piper...)
Affinity DataKi:  0.492nMAssay Description:SIK2, SIK1, SIK3, Abl, Scr, and EPHA2 assays were performed using an IMAP fluorescence polarization assay format (Molecular Devices Inc.). 06-13nM of...More data for this Ligand-Target Pair
Ligand Info
In Depth
Date in BDB:
1/21/2020
Entry Details
US Patent

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