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TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM130909(US8822500, Stauro- sporine | US9920060, Staurospor...)
Affinity DataIC50: 2.30nMAssay Description:Inhibition of human BRSK2 using KKLNRTLSFAEPG 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 BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 2.30nMAssay Description:Inhibition of human BRSK2 using KKLNRTLSFAEPG as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 3.30nMAssay Description:Inhibition of human BRSK2 using KKLNRTLSFAEPG 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 BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataKd:  3.5nMAssay Description:Binding constant for BRSK2 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataKd:  3.5nMAssay Description:Binding constant for full-length BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM31096(CHEMBL290084 | Staurosporine | cid_451705 | US2024...)
Affinity DataKd:  3.5nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM329334((2R)-2-(4-fluorophenyl)-N-[4-(2-{[2-methoxy-4-(met...)
Affinity DataKd:  4nMAssay Description:Binding affinity to BRSK2 (unknown origin) assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
LigandPNGBDBM387083(4-(4-(1-(3-Fluoronaphthalen-2-yl)-7-oxo-3-(trifluo...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM19023(BMS-562247 | CHEMBL231779 | 1-(4-methoxyphenyl)-7-...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387049(4-(4-(1-(4-Methoxyphenyl)-7-oxo-3-(trifluoromethyl...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387058(1-(4-Methoxyphenyl)-7-oxo-6-(1-(3-oxomorpholino)pi...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387056(1-(4-Methoxyphenyl)-7-oxo-6-(2′-oxo-[1,1R...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387057(N′-Cyano-1-(4-methoxyphenyl)-7-oxo-6-(2̸...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387068(1-(4-Methoxyphenyl)-7-oxo-6-(2-oxo-[1,4′-bip...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387082(4-(4-(1-(3-Fluoro-4-methoxyphenyl)-7-oxo-3-(triflu...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387078(4-(4-(1-(6-Chloronaphthalen-2-yl)-7-oxo-3-(trifluo...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387054(1-(4-Methoxyphenyl)-6-(1-(2-oxopyrrolidin-1-yl)pip...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387065(1-(4-(Difluoromethoxy)phenyl)-7-oxo-6-(1-(3-oxomor...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387080(4-(4-(1-(3-Aminobenzo[d]isoxazol-5-yl)-7-oxo-3-(tr...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387055(1-(4-Methoxyphenyl)-7-oxo-6-(2′-oxo-[1,1R...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387077(4-(4-(1-(4-(Difluoromethoxy)phenyl)-7-oxo-3-(trifl...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387050(1-(4-Methoxyphenyl)-6-(2′-oxo-[1,1′-bi...)
Affinity DataKi: <10nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50308060(CEP-701 | 16-hydroxy-16-(hydroxymethyl)-15-methyl-...)
Affinity DataKd:  16nMAssay Description:Binding affinity to BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2011
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50308060(CEP-701 | 16-hydroxy-16-(hydroxymethyl)-15-methyl-...)
Affinity DataKd:  16nMAssay Description:Binding constant for BRSK2 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM387085(3-(7-Oxo-6-(1-(3-oxomorpholino)piperidin-4-yl)-3-(...)
Affinity DataKi:  30nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387059(US9938272, Example 8b | US9938272, Example 8a)
Affinity DataKi:  30nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

LigandPNGBDBM387069(1-(4-Methoxyphenyl)-N5-(1-(3-oxomorpholino)piperid...)
Affinity DataKi:  30nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM36409(CID24905147 | 2-(4-amino-1-isopropyl-1H-pyrazolo[3...)
Affinity DataKd:  42nMAssay Description:Binding constant for BRSK2 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50395272(CHEMBL1231206)
Affinity DataIC50: 90nMAssay Description:Inhibition of BrSK2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50273571(Hesperadin | TCMDC-135395 | N-(2-oxo-3-(phenyl(4-(...)
Affinity DataKd:  92nMAssay Description:Binding affinity to human BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50307127((Z)-N,N-dimethyl-2-oxo-3-((4,5,6,7-tetrahydro-1H-i...)
Affinity DataIC50: 100nMAssay Description:Inhibition of BRSK2 in the presence of 50uM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/24/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 125nMAssay Description:Inhibition of human BRSK2 using KKLNRTLSFAEPG as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM482158(TAE684 | BDBM50242742)
Affinity DataKd:  190nMAssay Description:Binding constant for BRSK2 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM387064(7-Oxo-6-(1-(3-oxomorpholino)piperidin-4-yl)-1-(4-(...)
Affinity DataKi:  525nMAssay Description:Prothrombinase Assay:The effect of test compounds on prothrombinase activity is measured via thrombin generation. Briefly, 12.5 μL human factor ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2020
Entry Details
US Patent

TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50326053(PKC-412 | CHEMBL608533 | US20240132489, Compound S...)
Affinity DataKd:  650nMAssay Description:Binding constant for BRSK2 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50326053(PKC-412 | CHEMBL608533 | US20240132489, Compound S...)
Affinity DataKd:  650nMAssay Description:Binding constant for full-length BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM31094(PKC-412 | cid_24202429)
Affinity DataKd:  650nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50326053(PKC-412 | CHEMBL608533 | US20240132489, Compound S...)
Affinity DataKd:  650nMAssay Description:Binding affinity to BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2011
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM4814(SUNITINIB MALATE | CHEMBL535 | N-[2-(diethylamino)...)
Affinity DataKd:  1.10E+3nMAssay Description:Binding affinity to BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/11/2011
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM4814(SUNITINIB MALATE | CHEMBL535 | N-[2-(diethylamino)...)
Affinity DataKd:  1.10E+3nMAssay Description:Binding constant for BRSK2 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50298223(CHEMBL576817 | CHEMBL1240885 | CGP-57380 | N-(4-fl...)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of BRSK2 in the presence of 50uM ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/24/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM4814(SUNITINIB MALATE | CHEMBL535 | N-[2-(diethylamino)...)
Affinity DataKd:  1.10E+3nMAssay Description:Binding constant for full-length BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM4814(SUNITINIB MALATE | CHEMBL535 | N-[2-(diethylamino)...)
Affinity DataKd:  1.10E+3nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50355496(CHEMBL1908397)
Affinity DataKd:  1.20E+3nMAssay Description:Binding constant for BRSK2 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM25084(JMC504279 Compound 6 | 3-[2,4-diamino-6-(3-hydroxy...)
Affinity DataKd:  1.20E+3nMAssay Description:Binding constant for BRSK2 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50401900(CHEMBL2207198)
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50463483(CHEMBL4245242)
Affinity DataKi: >2.00E+3nMAssay Description:Inhibition of Brsk2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  2.70E+3nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM6866(1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b ...)
Affinity DataKd:  2.70E+3nMAssay Description:Binding constant for full-length BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase BRSK2(Human)
Center for Lymphoid Malignancies

Curated by ChEMBL
LigandPNGBDBM50401899(CHEMBL2207208)
Affinity DataIC50: 3.70E+3nMAssay Description:Inhibition of BRSK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
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