BDBM149404 AVL-301::CHEMBL3545308::CNX-419::CO-1686::Rociletinib::Tube721::US10167264, Compound CO-1686::US10300058, CO-1686::US10434101, Compound I-4::US11096942, Compound I-4::US8975249, I-4::US9783524, CO-1686

SMILES CC(=O)N1CCN(CC1)c2ccc(c(c2)OC)Nc3ncc(c(n3)Nc4cccc(c4)NC(=O)C=C)C(F)(F)F

InChI Key InChIKey=HUFOZJXAKZVRNJ-UHFFFAOYSA-N

Data  2 KI  60 IC50  1 Kd  1 EC50

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 64 hits for monomerid = 149404   

TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1.60E+3nMAssay Description:Inhibition of EGF-stimulated wild-type EGFR phosphorylation in human A549 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by san...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 262nMAssay Description:Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/10/2018
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 145nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [T790M](Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 2.10nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 180nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [T790M](Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1.30nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 180nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [T790M](Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1.30nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1.53E+5nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [T790M](Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 2.50E+3nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 460nMAssay Description:Inhibition of recombinant wild type human EGFR (695 to end residues) using Poly (4:1 Glu, Tyr) as substrate after 1 hr by ADP-Glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/27/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
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
In Depth
Date in BDB:
12/29/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 9nMAssay Description:Inhibition of EGFR T790M/exon 19 deletion mutant phosphorylation in human PC9-DRH cells preincubated for 2 hrs followed by EGF stimulation for 10 min...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 79nMAssay Description:Inhibition of EGFR exon 19 deletion mutant phosphorylation in human PC9 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandw...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 16nMAssay Description:Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by s...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReceptor tyrosine-protein kinase erbB-3(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 46nMAssay 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)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 20nMAssay Description:Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system using Poly(Glu,Tyr)4:1 as substr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 5.5nMAssay Description:Briefly, 10× stocks of EGFR-WT (PV3872) from Invitrogen and EGFR-T790M/L858R (40350) from BPS Bioscience, San Diego, Calif., 1.13×ATP (AS001A) and ap...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [T790M,L858R](Human)
Celgene Car

US Patent
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1nMAssay Description:Briefly, 10× stocks of EGFR-WT (PV3872) from Invitrogen and EGFR-T790M/L858R (40350) from BPS Bioscience, San Diego, Calif., 1.13×ATP (AS001A) and ap...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 3nMAssay Description:Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system preincubated for 30 mins followe...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/29/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
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
In Depth
Date in BDB:
12/29/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 500nMAssay Description:Inhibition of wild type N-terminal GST tagged human recombinant EGFR (695 to end amino acids) expressed in baculovirus infected Sf9 insect cells usin...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 20nMAssay Description:Inhibition of N-terminal GST tagged human recombinant EGFR L858R/T790M mutant (695 to end amino acids) expressed in baculovirus infected Sf9 insect c...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 5.5nMAssay Description:Briefly, 10× stocks of EGFR-WT (PV3872) from Invitrogen and EGFR-T790M/L858R (40350) from BPS Bioscience, San Diego, Calif., 1.13×ATP (AS001A) and ap...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/6/2022
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [T790M,L858R](Human)
Celgene Car

US Patent
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1nMAssay Description:Briefly, 10× stocks of EGFR-WT (PV3872) from Invitrogen and EGFR-T790M/L858R (40350) from BPS Bioscience, San Diego, Calif., 1.13×ATP (AS001A) and ap...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/6/2022
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 76nMAssay Description:Inhibition of wild type EGFR (unknown origin) in presence of ATP preincubated 5 mins measured for 30 mins by detection reagent based HTRF analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1.80nMAssay Description:Inhibition of recombinant human EGFR T790M/L858R mutant expressed in baculovirus insect cell expression system in presence of ATP preincubated 5 mins...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 77nMAssay Description:Inhibition of wild type EGFR (unknown origin) incubated for 10 mins by HTRF KinEASE-TK assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 4.20nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin) incubated for 35 mins by HTRF KinEASE-TK assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1.98E+3nMAssay Description:Inhibition of EGR-induced EGFR phosphorylation in human A549 cells pretreated for 2 hrs followed by EGF stimulation by immune assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 20nMAssay Description:Inhibition of EGFR L858R/T790M (unknown origin) incubated for 60 mins in presence of ATP by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 25nMAssay Description:Inhibition of EGFR (unknown origin) incubated for 60 mins in presence of ATP by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [L858R](Human)
Betta Pharmaceuticals

US Patent
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 0.460nMAssay Description:TBDMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2018
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 5.5nMpH: 7.5Assay Description:Briefly, 10x stocks of EGFR-WT (PV3872) from Invitrogen and EGFR-T790M/L858R (40350) from BPS Bioscience, San Diego, Calif., 1.13xATP (AS001A) and ap...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/3/2015
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1nMpH: 7.5Assay Description:Briefly, 10x stocks of EGFR-WT (PV3872) from Invitrogen and EGFR-T790M/L858R (40350) from BPS Bioscience, San Diego, Calif., 1.13xATP (AS001A) and ap...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/3/2015
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 2nMAssay Description:Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/18/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 1.60E+3nMAssay Description:Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 16nMAssay 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
In Depth
Date in BDB:
7/23/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 9nMAssay 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
In Depth
Date in BDB:
7/23/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 46nMAssay Description:Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 79nMAssay Description:Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 65nMAssay Description:Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/23/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 62nMAssay Description:Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/27/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 187nMAssay Description:Inhibition of EGFR Del ex19 mutant phosphorylation in human HCC827 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/27/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 211nMAssay Description:Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/27/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 4.33E+3nMAssay Description:Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/27/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of wild type EGFR phosphorylation in human H1299 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/27/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/27/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 272nMAssay Description:Inhibition of recombinant human GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus expression system using Poly(Glu,Tyr)4:1 as substrate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor [T790M](Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM149404(US8975249, I-4 | CO-1686 | Rociletinib | AVL-301 |...)
Affinity DataIC50: 412nMAssay Description:TBDMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2018
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
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