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TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304254(US10143695, Compound 78)
Affinity DataIC50: 0.0600nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM13530(cid_5291 | STI571 | N-(4-methyl-3-{[4-(pyridin-3-y...)
Affinity DataIC50: 0.0600nMAssay Description:Inhibition of HER2 (unknown origin) incubated for 1 hr in presence of ATP by Kinase-Glo Plus luminescence kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/26/2023
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304255(US10143695, Compound 79)
Affinity DataIC50: 0.0900nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
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)
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-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304241(US10143695, Compound 8A)
Affinity DataIC50: 0.140nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM50606784(CHEMBL5221067)
Affinity DataIC50: 0.140nMAssay Description:Inhibition of HER2 (unknown origin) incubated for 1 hr in presence of ATP by Kinase-Glo Plus luminescence kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/26/2023
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304240(US10143695, Compound 7A)
Affinity DataIC50: 0.150nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304234(US10143695, Compound 8)
Affinity DataIC50: 0.150nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2 [V777L](Homo sapiens (Human))
Shanghai Pharmaceuticals Holding

Curated by ChEMBL
LigandPNGBDBM50604493(CHEMBL5178703)
Affinity DataIC50: 0.160nMAssay Description:Inhibition of HER2 V777L mutant (unknown origin) incubated for 120 mins in presence of 33P-ATP by P81 ion exchange cellulose chromatographyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304245(US10143695, Compound 28)
Affinity DataIC50: 0.160nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304257(US10143695, Compound 83)
Affinity DataIC50: 0.180nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

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-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304242(US10143695, Compound 19)
Affinity DataIC50: 0.200nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304246(US10143695, Compound 13A)
Affinity DataIC50: 0.280nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304254(US10143695, Compound 78)
Affinity DataIC50: 0.290nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304240(US10143695, Compound 7A)
Affinity DataIC50: 0.300nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304247(US10143695, Compound 48)
Affinity DataIC50: 0.300nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
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:  0.300nMAssay 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)
TargetReceptor tyrosine-protein kinase erbB-2 [1-775,'YVMA',776-1255](Human)
Korea Reserarch Institute of Chemical Technology

US Patent
LigandPNGBDBM700904(N-(5-amino-4-methoxy-2- (methyl(2-(piperidin-1- yl...)
Affinity DataIC50: 0.300nMAssay Description:The activity of the compounds of the present invention against HER mutant enzymes was measured using the HTRF system purchased by Cisbio as follows. ...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
2/23/2025
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM50648260(CHEMBL5614250)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of HER-2 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
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
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304255(US10143695, Compound 79)
Affinity DataIC50: 0.310nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM581371(US11505527, Compound 4j)
Affinity DataIC50: 0.340nMAssay Description:An in vitro kinase assay was performed to evaluate the kinase suppression activity of the most promising cytotoxic candidates 4b, 4j against four dif...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/21/2023
Entry Details
US Patent

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
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304242(US10143695, Compound 19)
Affinity DataIC50: 0.350nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

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
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304235(US10143695, Compound 12)
Affinity DataIC50: 0.400nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

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-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM50604493(CHEMBL5178703)
Affinity DataIC50: 0.420nMAssay Description:Inhibition of HER2 D769H mutant (unknown origin) incubated for 120 mins in presence of 33P-ATP by P81 ion exchange cellulose chromatographyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM50604493(CHEMBL5178703)
Affinity DataIC50: 0.430nMAssay Description:Inhibition of HER2 D769Y mutant (unknown origin) incubated for 120 mins in presence of 33P-ATP by P81 ion exchange cellulose chromatographyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304234(US10143695, Compound 8)
Affinity DataIC50: 0.430nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM50030383(CHEMBL3344216)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of HER2 (unknown origin) assessed as reduction in autophosphorylation by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/10/2016
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM50182688(N-[4-[(3-bromo-4-fluorophenyl)amino]pyrido[3,4-d]p...)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cellsMore 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
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM50182684(N-[4-[(3-bromo-4-fluorophenyl)amino]pyrido[3,4-d]p...)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of erbB2 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-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM304241(US10143695, Compound 8A)
Affinity DataIC50: 0.550nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM16673(Xarelto | BAY439006 | CHEMBL1336 | BAY 43-9006 | 4...)
Affinity DataIC50: 0.560nMAssay Description:An in vitro kinase assay was performed to evaluate the kinase suppression activity of the most promising cytotoxic candidates 4b, 4j against four dif...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/21/2023
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-2(Human)
Mersana Therapeutics

US Patent
LigandPNGBDBM50604493(CHEMBL5178703)
Affinity DataIC50: 0.560nMAssay Description:Inhibition of HER2 R896C mutant (unknown origin) incubated for 120 mins in presence of 33P-ATP by P81 ion exchange cellulose chromatographyMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
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)
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