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TargetSerine/threonine-protein kinase B-raf(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50452149(CHEMBL4216073)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of recombinant C-terminal his6-tagged B-Raf (437 to 765 residues) V600E mutant (unknown origin) catalytic domain expressed in baculovirus ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetSerine/threonine-protein kinase B-raf(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50452150(CHEMBL4216386)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of recombinant C-terminal his6-tagged B-Raf (437 to 765 residues) V600E mutant (unknown origin) catalytic domain expressed in baculovirus ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM213578(US9278981, 170)
Affinity DataIC50: <0.300nMAssay Description:Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase B-raf(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50452152(CHEMBL4217462)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of recombinant C-terminal his6-tagged B-Raf (437 to 765 residues) V600E mutant (unknown origin) catalytic domain expressed in baculovirus ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM213594(US9278981, 186)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50459091(ABL-001 | ABL001 | ABL001-NX | Asciminib | NVP-ABL...)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM213656(US9278981, 248)
Affinity DataIC50:  0.5nMAssay Description:Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50459090(CHEMBL4213152)
Affinity DataIC50:  0.700nMAssay Description:Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetProtein kinase C alpha type(Human)
Novartis

LigandPNGBDBM33970(maleimide derivative, 12)
Affinity DataIC50:  0.900nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase B-raf(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50452147(CHEMBL4204192)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of recombinant C-terminal his6-tagged B-Raf (437 to 765 residues) V600E mutant (unknown origin) catalytic domain expressed in baculovirus ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223939(6-(4-methoxybenzyl)-7-neopentyl-7H-pyrrolo[2,3-d]p...)
Affinity DataIC50:  1nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C theta type(Human)
Novartis

LigandPNGBDBM33971(AEB071 | Sotrastaurin | med.21724, Compound 190)
Affinity DataIC50:  1nMT: 25°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223914(6-((4-(4-fluorophenyl)piperazin-1-yl)methyl)-7-neo...)
Affinity DataIC50:  1nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetHistamine H1 receptor(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50112349(CHEMBL3609328)
Affinity DataIC50:  1nMAssay Description:Inhibition of recombinant human histamine H1 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50459089(CHEMBL4217559)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223921(6-(4-(benzo[d][1,3]dioxol-5-yl)benzyl)-7-neopentyl...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223935(CHEMBL399842 | N-(4-((2-cyano-7-neopentyl-7H-pyrro...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223915(6-benzyl-7-neopentyl-7H-pyrrolo[2,3-d]pyrimidine-2...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C delta type(Human)
Novartis

LigandPNGBDBM33971(AEB071 | Sotrastaurin | med.21724, Compound 190)
Affinity DataIC50:  1.30nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223925(6-(4-((4-methylpiperazin-1-yl)methyl)benzyl)-7-cyc...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM230760(US9340537, 14 | US9896444, Example 14)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetProtein kinase C beta type(Human)
Novartis

LigandPNGBDBM2683(2-[1-(3-dimethylaminopropyl)-indol-3-yl]-3-(indol-...)
Affinity DataIC50:  1.60nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223919(7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[ind...)
Affinity DataIC50:  1.70nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C beta type(Human)
Novartis

LigandPNGBDBM33970(maleimide derivative, 12)
Affinity DataIC50:  1.80nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C beta type(Human)
Novartis

LigandPNGBDBM33971(AEB071 | Sotrastaurin | med.21724, Compound 190)
Affinity DataIC50:  2nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetMitogen-activated protein kinase 11/12/13/14(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50452152(CHEMBL4217462)
Affinity DataIC50:  2nMAssay Description:Inhibition of P38 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetMitogen-activated protein kinase 11/12/13/14(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50452151(CHEMBL4208527)
Affinity DataIC50:  2nMAssay Description:Inhibition of P38 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetProto-oncogene tyrosine-protein kinase Src(Human)
Novartis Institute of Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50320214(3-(7-amino-3-(4-(4-methylpiperazin-1-yl)phenyl)pyr...)
Affinity DataIC50:  2nMAssay Description:Inhibition of SRCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C eta type(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50391897(CHEMBL2147537)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant human PKCeta assessed as [33P]-ATP incorporation into tridecapeptide substrate after 60 mins by scintillation proximity ass...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C beta type(Human)
Novartis

LigandPNGBDBM33968(maleimide derivative, 10)
Affinity DataIC50:  2.10nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C alpha type(Human)
Novartis

LigandPNGBDBM33971(AEB071 | Sotrastaurin | med.21724, Compound 190)
Affinity DataIC50:  2.10nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedMMDB
PDB3D3D Structure (crystal)

TargetProtein kinase C alpha type(Human)
Novartis

LigandPNGBDBM33968(maleimide derivative, 10)
Affinity DataIC50:  2.20nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223910(6-(4-chlorobenzyl)-7-cyclohexyl-7H-pyrrolo[2,3-d]p...)
Affinity DataIC50:  2.30nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM213441(US9278981, 33)
Affinity DataIC50:  2.30nMAssay Description:Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetProtein kinase C alpha type(Human)
Novartis

LigandPNGBDBM2683(2-[1-(3-dimethylaminopropyl)-indol-3-yl]-3-(indol-...)
Affinity DataIC50:  2.30nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetSerine/threonine-protein kinase B-raf(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50452151(CHEMBL4208527)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant C-terminal his6-tagged B-Raf (437 to 765 residues) V600E mutant (unknown origin) catalytic domain expressed in baculovirus ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223911(7-neopentyl-6-((pyridin-4-yloxy)methyl)-7H-pyrrolo...)
Affinity DataIC50:  3nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C theta type(Human)
Novartis

LigandPNGBDBM33968(maleimide derivative, 10)
Affinity DataIC50:  3.30nMT: 25°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223920(6-(4-morpholinobenzyl)-7-cyclohexyl-7H-pyrrolo[2,3...)
Affinity DataIC50:  3.40nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50156086(9-CYCLOPENTYL-6-[2-(3-IMIDAZOL-1-YL-PROPOXY)-PHENY...)
Affinity DataIC50:  3.5nMAssay Description:Inhibitory concentration against recombinant human cathepsin K by using Z-Phe-Arg-AMC as synthetic substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank
PDB3D3D Structure (crystal)

TargetEpithelial discoidin domain-containing receptor 1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50237710(4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifl...)
Affinity DataIC50:  3.70nMAssay Description:Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase ABL1(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM213443(US9278981, 35)
Affinity DataIC50:  4nMAssay Description:Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMedPDB3D3D Structure (crystal)

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223940(6-((4,5-dichloro-1H-imidazol-1-yl)methyl)-7-neopen...)
Affinity DataIC50:  4nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223936(6-((5,5-dimethyl-2,4-dioxooxazolidin-3-yl)methyl)-...)
Affinity DataIC50:  4nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase Lck(Human)
Novartis Institute of Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50320205(CHEMBL1083001 | N-(4-(7-amino-3-(4-(4-methylpipera...)
Affinity DataIC50:  4nMAssay Description:Inhibition of LCKMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C eta type(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50391902(CHEMBL2147542)
Affinity DataIC50:  4nMAssay Description:Inhibition of recombinant human PKCeta assessed as [33P]-ATP incorporation into tridecapeptide substrate after 60 mins by scintillation proximity ass...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetTyrosine-protein kinase Lck(Human)
Novartis Institute of Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50320225(CHEMBL1085316 | N-(4-(7-amino-3-(3-(4-methylpipera...)
Affinity DataIC50:  4nMAssay Description:Inhibition of LCKMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C delta type(Human)
Novartis

LigandPNGBDBM33968(maleimide derivative, 10)
Affinity DataIC50:  4.40nMpH: 7.4 T: 23°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetCathepsin K(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50223941(6-(4-((diethylamino)methyl)benzyl)-7-cyclohexyl-7H...)
Affinity DataIC50:  4.70nMAssay Description:Inhibition of cathepsin K by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

TargetProtein kinase C theta type(Human)
Novartis

LigandPNGBDBM33970(maleimide derivative, 12)
Affinity DataIC50:  4.80nMT: 25°CAssay Description:Classical and novel PKC isotypes were assayed by scintillation proximity assay technology. In brief, the assay was performed in reaction buffer by in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed

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