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TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of EGFR deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of EGFR T790M/L858R mutant (unknown origin) by high-throughput biochemical screeningMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/12/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM4779(cid_156414 | PD0183805 | CHEMBL545315 | CHEMBL3196...)
Affinity DataKi:  0.110nMAssay Description:Reversible binding affinity to human EGFR L858R/ T790M double mutant expressed in baculovirus by fluorometric analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50383274(CHEMBL1229592 | US9670213, WZ4002 | US10167264, WZ...)
Affinity DataIC50: 0.190nMAssay Description:Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) T790M/L858R mutant expressed in Sf9 cells pre-incubated fo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/4/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50123453(CHEMBL3623290)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of EGFR exon19 deletion mutant (unknown origin) by HTRF assay in presence of Km of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50123453(CHEMBL3623290)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin) by HTRF assay in presence of Km of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/9/2016
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5447(ZD1839 | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141636(CHEMBL3758502)
Affinity DataKi:  0.200nMAssay Description:Inhibition of EGFR deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataKi:  0.300nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataKi:  0.300nMAssay Description:Inhibition of EGFR T790M/del746 to 750 mutant (unknown origin) by high-throughput biochemical screeningMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/12/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50183383(CHEMBL3818547)
Affinity DataIC50: 0.310nMAssay Description:Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/29/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50183406(CHEMBL3818062)
Affinity DataIC50: 0.350nMAssay Description:Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/29/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50183388(CHEMBL3818015)
Affinity DataIC50: 0.380nMAssay Description:Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/29/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141902(CHEMBL3758602)
Affinity DataKi:  0.400nMAssay Description:Inhibition of EGFR deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50166941(CHEMBL3797606)
Affinity DataIC50: 0.400nMAssay 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
In Depth
Date in BDB:
8/22/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50383274(CHEMBL1229592 | US9670213, WZ4002 | US10167264, WZ...)
Affinity DataIC50: 0.420nMAssay Description:Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) L858R mutant expressed in Sf9 cells pre-incubated for 30 m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/4/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141610(CHEMBL3759096)
Affinity DataKi: <0.5nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141610(CHEMBL3759096)
Affinity DataKi: <0.5nMAssay Description:Inhibition of EGFR deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141636(CHEMBL3758502)
Affinity DataKi:  0.5nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50322823((S)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahy...)
Affinity DataIC50: 0.570nMAssay 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
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of EGFR T790M mutant (unknown origin) incubated for 1 hr by spectrophotometric analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/26/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM112499(DACOMITINIB | US8623883, No. 2 | WO2022090481, Exa...)
Affinity DataIC50: 0.630nMAssay 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
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM5447(ZD1839 | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[...)
Affinity DataIC50: 0.637nMAssay Description:Inhibition of cytoplasmic GST-tagged human recombinant EGFR L858R mutant expressed in baculovirus system by z-lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/9/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50383274(CHEMBL1229592 | US9670213, WZ4002 | US10167264, WZ...)
Affinity DataIC50: 0.660nMAssay Description:Inhibition of EGFR T790M/L858R double mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM195875(US9670213, Compound 020 N-(3-(2-(4-(4-methyl-1-pip...)
Affinity DataIC50: 0.677nMAssay Description:Inhibition of EGFR T790M/L858R double mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50166942(CHEMBL3798501)
Affinity DataIC50: 0.700nMAssay 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
In Depth
Date in BDB:
8/22/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50183391(CHEMBL3818563)
Affinity DataIC50: 0.710nMAssay Description:Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/29/2017
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM4552(CHEMBL288441 | SKI-606 | 4-[(2,4-Dichloro-5-methox...)
Affinity DataKd:  0.770nMAssay Description:Binding constant for ERBB3 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50383274(CHEMBL1229592 | US9670213, WZ4002 | US10167264, WZ...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of EGFR L858R/T90M double mutant (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50183395(CHEMBL3818289)
Affinity DataIC50: 0.830nMAssay Description:Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/29/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50131843(CHEMBL3633152)
Affinity DataKd:  0.960nMAssay Description:Competitive binding affinity to human EGFR T790M mutant in presence of immobilized ligandMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2016
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50322823((S)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahy...)
Affinity DataIC50: 0.970nMAssay Description:Inhibition of wild type EGFR T790M mutant (unknown origin) incubated for 5 mins by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReceptor tyrosine-protein kinase erbB-3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50210162(CHEMBL3883534)
Affinity DataIC50: 1nMAssay Description:Inhibition of EGFR L858R mutant phosphorylation in human H3255 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50177903(CHEMBL3814825)
Affinity DataIC50: 1nMAssay Description:Inhibition of recombinant N-terminal GST-tagged human EGFR T790M/L858R double mutant using biotinylated TK substrate incubated for 50 mins by HTRF as...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/17/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM2579(CHEMBL388978 | Staurosporine, 8 | Staurosporin, 4 ...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of EGFR T790M/L858R mutant (unknown origin) incubated for 1 hr by spectrophotometric analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/26/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM195887(US9670213, Compound 032 N-(3-(2-(2-methoxy-4-(4-me...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of EGFR T790M/L858R double mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50498986(CHEMBL3736121)
Affinity DataKi:  1.10nMAssay Description:Inhibition of human EGFR T790M/L858R double mutant using Fl-EEPLYWSFPAKKK-CONH2 as substrate preincubated for 30 mins followed by addition of substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2020
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50461172(CHEMBL4228518)
Affinity DataIC50: 1.20nMAssay 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 Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141902(CHEMBL3758602)
Affinity DataKi:  1.30nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141902(CHEMBL3758602)
Affinity DataKi:  1.30nMAssay Description:Inhibition of EGFR T790M/deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM195875(US9670213, Compound 020 N-(3-(2-(4-(4-methyl-1-pip...)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2020
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141636(CHEMBL3758502)
Affinity DataKi:  1.60nMAssay Description:Inhibition of EGFR T790M/deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50461178(CHEMBL4225777)
Affinity DataIC50: 1.70nMAssay 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 Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141611(CHEMBL3758739)
Affinity DataKi:  1.70nMAssay Description:Inhibition of EGFR deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50166944(CHEMBL3799864)
Affinity DataIC50: 1.80nMAssay 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
In Depth
Date in BDB:
8/22/2017
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50461174(CHEMBL4226676)
Affinity DataIC50: 1.90nMAssay 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 Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50450868(CHEMBL4216679)
Affinity DataIC50: 2nMAssay Description:Inhibition of EGFR L858R mutant phosphorylation in human H3255 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50112173(CHEMBL3608429)
Affinity DataIC50: 2nMAssay Description:Inhibition of EGFR L858R mutant phosphorylation in human H3255 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-3(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50461179(CHEMBL4226151)
Affinity DataIC50: 2nMAssay 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 Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetEpidermal growth factor receptor(Human)
Genentech

Curated by ChEMBL
LigandPNGBDBM50141667(CHEMBL3759499)
Affinity DataKi:  2nMAssay Description:Inhibition of EGFR T790M/L858R mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/6/2017
Entry Details Article
PubMed
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