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TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM373712(US10246444, Example 92)
Affinity DataIC50: 0.0300nMAssay Description:Inhibition of HER4 (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50357312(IBRUTINIB | US9181263, 1 | US9108973, Ref 1 | US92...)
Affinity DataIC50: 0.100nMAssay Description:IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 uM ATP.). Reaction condition...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/3/2017
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM698784(US20240317756, Compound 1)
Affinity DataIC50: 0.100nMAssay Description:For enzyme inhibition assays, compounds were tested in range of ten concentrations from 10 uM to 0.0005 uM using purified enzymes and the Hotspot kin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/28/2025
Entry Details
US Patent

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)
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50357312(IBRUTINIB | US9181263, 1 | US9108973, Ref 1 | US92...)
Affinity DataIC50: 0.100nMAssay Description:IC50s were determined using the in vitro HotSpot kinase assay (purified enzymes, 33P-ATP, an appropriate substrate and 1 μM ATP.). For enzyme in...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/6/2016
Entry Details
US Patent

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
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM373723(US10246444, Example 90)
Affinity DataIC50: 0.190nMAssay Description:Inhibition of HER4 (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
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
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50357312(IBRUTINIB | US9181263, 1 | US9108973, Ref 1 | US92...)
Affinity DataIC50: 0.25nMAssay Description:Inhibition of human HER4 using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50357312(IBRUTINIB | US9181263, 1 | US9108973, Ref 1 | US92...)
Affinity DataIC50: 0.25nMAssay Description:Inhibition of human HER4 using poly[Glu:Tyr] (4:1) as substrate preincubated for 60 mins followed by [gamma-33P]-ATP addition and measured after 120 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
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)
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM373725(US10246444, Example 98)
Affinity DataIC50: 0.450nMAssay Description:Inhibition of HER4 (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50182693(N-[4-[(3-chloro-4-fluorophenyl)amino]pyrido[3,4-d]...)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of erbB4 fusion protein expressed in baculovirus by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/6/2012
Entry Details Article
PubMed
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)
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50455738(CHEMBL4211949)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of recombinant human ErbB4 using Poly(Glu, Tyr) 4:1 as substrate after 1 hr by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50357312(IBRUTINIB | US9181263, 1 | US9108973, Ref 1 | US92...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of HER4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMed
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-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50182684(N-[4-[(3-bromo-4-fluorophenyl)amino]pyrido[3,4-d]p...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of erbB4 fusion protein expressed in baculovirus by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/6/2012
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50652893(Allitinib | Als 1306 | Ast 1306 | Ast-1306 | Ast13...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of ErbB4 (unknown origin) using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins by ELISAMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
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
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50357312(IBRUTINIB | US9181263, 1 | US9108973, Ref 1 | US92...)
Affinity DataKd:  0.910nMAssay Description:Binding affinity to ERBB4 (unknown origin) assessed as dissociation constant by KINOMEscan analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
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-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50191486(CHEMBL3959248)
Affinity DataIC50: 1nMAssay Description:Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assesse...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/26/2018
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50322823((S)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahy...)
Affinity DataIC50: 1nMAssay Description:Inhibition of HER4 (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50182682(N-[4-[(3-chloro-4-fluorophenyl)amino]pyrido[3,4-d]...)
Affinity DataIC50: 1nMAssay Description:Inhibition of erbB4 fusion protein expressed in baculovirus by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/6/2012
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50331095(Tivozanib | CHEMBL1289494 | US10464902, Tivozanib)
Affinity DataIC50: 1nMAssay Description:Inhibition of ErbB4 (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Sabila Biosciences

Curated by ChEMBL
LigandPNGBDBM50322823((S)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahy...)
Affinity DataIC50: 1nMAssay Description:Inhibition of HER4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
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