BDBM50029668 AZD-9291::Osimertinib::US10085983, Compound AZD-9291::US10227342, Example 24::US11111233, Example AZD9291::US20230322822, Compound AZD9291::US9890168, Compound AZD-9291::WO2022090481, Example osimertinib

SMILES COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1cn(C)c2ccccc12

InChI Key InChIKey=DUYJMQONPNNFPI-UHFFFAOYSA-N

Data  7 KI  206 IC50  21 EC50

PDB links: 10 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 206 hits for monomerid = 50029668   

TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  74nMAssay Description:Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA methodMore data for this Ligand-Target Pair
TargetInsulin receptor(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  912nMAssay Description:Inhibition of INSR (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  1.50E+4nMAssay Description:Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  1.70E+4nMAssay Description:Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  4.80E+5nMAssay Description:Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assayMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  1.62E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  2.90E+6nMAssay Description:Inhibition of IGF1R (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  150nMAssay Description:Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  15nMAssay Description:Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  13nMAssay Description:Inhibition of EGFR deletion/T790M mutant autophosphorylation in human PC9-DRH cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  36nMAssay Description:Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  56nMAssay Description:Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  23nMAssay Description:Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  409nMAssay Description:Inhibition of wild-type EGFR (unknown origin) expressed in baculovirus expression system after 1 hr by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  11nMAssay Description:Inhibition of EGFR T790M/L858R mutant (unknown origin) expressed in baculovirus expression system after 1 hr by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  480nMAssay Description:Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  17nMAssay Description:Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  15nMAssay Description:Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [668-1210,T790M,L858R](Homo sapiens (Human))
Shanghai Haiyan Pharmaceutical Technology

US Patent
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  2nMT: 2°CAssay Description:All reagents used in the following z′-lyte assay were purchased from Invitrogen.The inhibitory activity on T790M/L858R double mutant EGFR kinas...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  3nMT: 2°CAssay Description:All reagents used in the following z′-lyte assay were purchased from Invitrogen.The inhibitory activity on T790M/L858R double mutant EGFR kinas...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  260nMAssay Description:Inhibition of N-terminal 6His/TEV protease cleavage site-tagged wild type human EGFR using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of human N-terminal GST-fused EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubat...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of wild-type human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  109nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using Poly(Glu,Tyr) as substrate after 40 mins by Kinase-Glo luminescence assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  2.40nMAssay Description:Inhibition of EGFR L858R/T790M double mutant (unknown origin) using Poly(Glu,Tyr) as substrate after 40 mins by Kinase-Glo luminescence assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50: <1nMAssay Description:Inhibition of EGFR L858R/T790M double mutant (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  77nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of wild type EGFR (unknown origin) using Poly(Glu,Tyr) as substrate after 40 mins by Kinase-Glo luminescence assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin) using Poly(Glu,Tyr) as substrate after 40 mins by Kinase-Glo luminescence assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  2nMAssay Description:Inhibition of wild type EGFR (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  1nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  300nMAssay Description:A compound's ability in selectively inhibiting EGFR exon 20 insertion mutations can be assessed using Ba/F3 cells, a murine pro-B cell line, whic...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50: <100nMAssay Description:A compound's ability in selectively inhibiting EGFR exon 20 insertion mutations can be assessed using Ba/F3 cells, a murine pro-B cell line, whic...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M](Homo sapiens (Human))
Ariad Pharmaceuticals

US Patent
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50: <100nMAssay Description:A compound's ability in selectively inhibiting EGFR exon 19 deletion and T790M concurrent mutations can be assessed using Ba/F3 cells, a murine p...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M,L858R](Homo sapiens (Human))
Ariad Pharmaceuticals

US Patent
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50: <100nMAssay Description:A compound's ability in selectively inhibiting EGFR L858R and T790M concurrent mutations can be assessed using Ba/F3 cells, a murine pro-B cell l...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  750nMAssay Description:A compound's ability in selectively inhibiting Her2 exon 20 YVMA insertion mutations can be assessed using Ba/F3 cells, a murine pro-B cell line,...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  225nMAssay Description:Inhibition of wild-type EGFR (unknown origin) using Tyr 4 peptide as substrate in presence of ATP by Z-LYTE kinase assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  480nMAssay Description:Inhibition of EGF-stimulated wild type EGFR phosphorylation in human LoVo cells incubated for 2 hrs followed by EGF stimulation for 10 mins by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50: <0.5nMAssay Description:Inhibition of wild-type EGFR (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M,L858R](Homo sapiens (Human))
Ariad Pharmaceuticals

US Patent
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  2nMAssay Description:The inhibitory activities on T790M/L858R double mutant EGFR kinase (Invitrogen, PV4879) and wild-type EGFR kinase (Invitrogen, PV3872) were determine...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  3nMAssay Description:The inhibitory activities on T790M/L858R double mutant EGFR kinase (Invitrogen, PV4879) and wild-type EGFR kinase (Invitrogen, PV3872) were determine...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  2nMAssay Description:Inhibition of wild type N-terminal GST-fused human EGFR cytoplasmic domain expressed in baculovirus expression system preincubated for 30 mins follow...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  570nMAssay Description:Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  14nMAssay Description:Inhibition of human recombinant cytoplasmic GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated fo...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  12nMAssay Description:Inhibition of recombinant human GST-tagged EGFR T790M/L858R double mutant expressed in baculovirus expression system using poly (Glu, Tyr) 4:1 as sub...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  270nMAssay Description:Inhibition of recombinant human GST-tagged wild type EGFR expressed in baculovirus expression system using poly (Glu, Tyr) 4:1 as substrate after 1 h...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  11nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  13nMAssay Description:Inhibition of EGFR exon 19 deletion mutant (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Genentech

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  494nMAssay Description:Inhibition of wild-type EGFR (unknown origin)More data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-3(Homo sapiens (Human))
Xi'An Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50029668(AZD-9291 | Osimertinib | US10085983, Compound AZD-...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin) using poly (Glu, Tyr) as substrate after 40 mins by kinase-glo plus luminescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed