ChEMBL ligand: CHEMBL4650281 (Cln 081, Cln-081, CLN081, TAS-6417, TAS6417, TPC-064, TPC064, Zipalertinib)
epidermal growth factor receptor/Epidermal growth factor receptor in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL	Inhibition of wildtype EGFR (unknown origin) phosphorylation transfected in human NCI-H2073 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by ELISA	B	6.72	pIC50	190	nM	IC50	J Med Chem (2024) 67: 8988-9027 [PMID:38770784]
ChEMBL	Inhibition of wildtype EGFR (unknown origin) phosphorylation transfected in human NCI-H2073 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by HTRF assay	B	7.11	pIC50	77	nM	IC50	J Med Chem (2024) 67: 8988-9027 [PMID:38770784]
ChEMBL	Inhibition of EGFR D770_N771insSVD mutant (unknown origin) phosphorylation transfected in human NCI-H2073 cells incubated for 2 hrs by ELISA	B	7.24	pIC50	57	nM	IC50	J Med Chem (2024) 67: 8988-9027 [PMID:38770784]
ChEMBL	Inhibition of EGFR D770_N771insSVD mutant (unknown origin) phosphorylation transfected in human NCI-H2073 cells incubated for 2 hrs by HTRF assay	B	7.68	pIC50	21	nM	IC50	J Med Chem (2024) 67: 8988-9027 [PMID:38770784]
ChEMBL	Inhibition of wildtype EGFR (unknown origin) phosphorylation	B	8.1	pIC50	8	nM	IC50	J Med Chem (2023) 66: 11656-11671 [PMID:37669428]
GtoPdb	Inhibition of WT hEGFR in a biochemical enzyme assay	-	8.1	pIC50	8	nM	IC50	Mol Cancer Ther (2018) 17: 1648-1658 [PMID:29748209]
GtoPdb	Inhibition of hEGFR with D770_N771insNPG insertion in a biochemical enzyme assay	-	8.13	pIC50	7.4	nM	IC50	Mol Cancer Ther (2018) 17: 1648-1658 [PMID:29748209]
ChEMBL	Inhibition of EGFR-D770-N771insNPG mutant (unknown origin) phosphorylation	B	8.13	pIC50	7.4	nM	IC50	J Med Chem (2023) 66: 11656-11671 [PMID:37669428]
ChEMBL	Inhibition of recombinant wildtype human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in Sf21 insect cells using Poly(Glu,Tyr) peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 50 mins in presence of ATP by ADP-Glo reagent based assay	B	8.52	pIC50	<3	nM	IC50	J Med Chem (2024) 67: 8988-9027 [PMID:38770784]
ChEMBL	Inhibition of 6His-tagged TEV-GS fused EGFR D770_N771insNPG mutant (G696 to G1210 reisudes) (unknown origin) expressed in Sf21 cells using Poly(Glu,Tyr) peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins in presence of ATP by ADP-Glo reagent based assay	B	8.52	pIC50	<3	nM	IC50	J Med Chem (2024) 67: 8988-9027 [PMID:38770784]
GtoPdb	Inhibition of hEGFR with T790M/L858R mutation in a biochemical enzyme assay	-	8.7	pIC50	2	nM	IC50	Mol Cancer Ther (2018) 17: 1648-1658 [PMID:29748209]
ChEMBL	Inhibition of wild type EGFR (unknown origin)	B	8.96	pIC50	1.1	nM	IC50	RSC Med Chem (2022) 13: 1008-1028 [PMID:36324498]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]