ChEMBL ligand: CHEMBL3899754
kelch like ECH-associated protein 1/Kelch-like ECH-associated protein 1 in Human [ChEMBL: CHEMBL2069156] [GtoPdb: 2757] [UniProtKB: Q14145] kelch like ECH-associated protein 1/Kelch-like ECH-associated protein 1 in Mouse [ChEMBL: CHEMBL3562164] [GtoPdb: 2757] [UniProtKB: Q9Z2X8] 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
kelch like ECH-associated protein 1/Kelch-like ECH-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069156] [GtoPdb: 2757] [UniProtKB: Q14145]
GtoPdb	Binding affinity determined by ITC, between KEAP1 kelch domain and RA839.	-	5.22	pKd	6000	nM	Kd	J Biol Chem (2015) 290: 28446-55 [PMID:26459563]
ChEMBL	Inhibition of human Keap1 kelch domain binding to Nrf2-ETGE peptide by ITC assay	B	5.22	pKd	6000	nM	Kd	J Med Chem (2018) 61: 8088-8103 [PMID:29750408]
ChEMBL	Binding affinity to human KEAP1 Kelch domain (322 to 609 residues) by isothermal titration calorimetric method	B	5.22	pKd	6000	nM	Kd	J Med Chem (2019) 62: 6796-6813 [PMID:31283229]
ChEMBL	Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) using RA839 as titrant by isothermal titration calorimetry	B	5.22	pKd	6000	nM	Kd	J Med Chem (2019) 62: 8028-8052 [PMID:31411465]
ChEMBL	Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance analysis	B	6.33	pKd	470	nM	Kd	J Med Chem (2019) 62: 8028-8052 [PMID:31411465]
ChEMBL	Inhibition of Cys5-LDEETGEFL-NH2 binding to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) measured after 10 to 15 mins by fluorescence polarization assay	B	7.32	pKi	48	nM	Ki	J Med Chem (2019) 62: 8028-8052 [PMID:31411465]
GtoPdb	Inhibition constant determined using fluorescence polarization to monitor the interaction of human KEAP1 kelch domain (amino acids Ala321–Thr609) to a fluorescently labeled human Nrf2 peptide (Alexa633-AFFAQLQLDEETGEFL).	-	6.85	pIC50	~140	nM	IC50	J Biol Chem (2015) 290: 28446-55 [PMID:26459563]
ChEMBL	Inhibition of human Keap1 kelch domain binding to Nrf2-ETGE peptide preincubated for 15 mins followed by peptide addition measured after 30 mins by fluorescence polarization assay	B	6.85	pIC50	140	nM	IC50	J Med Chem (2018) 61: 8088-8103 [PMID:29750408]
ChEMBL	Displacement of FITC-LDEETGEFL-NH2 from human KEAP1 Kelch domain (322 to 609 residues) measured after 30 mins by fluorescence polarization assay	B	6.85	pIC50	140	nM	IC50	J Med Chem (2019) 62: 6796-6813 [PMID:31283229]
ChEMBL	Inhibition of Alexa633-AFFAQLQLDEETGEFL binding to recombinant human KEAP1 Kelch domain (321 to 609 residues) preincubated for 15 mins followed by Alexa633-AFFAQLQLDEETGEFL addition and measured after 30 mins by fluorescence polarization assay	B	6.85	pIC50	140	nM	IC50	J Med Chem (2019) 62: 8028-8052 [PMID:31411465]
ChEMBL	Inhibition of FITC-9mer Nrf2 peptide interaction with human recombinant Keap1 Kelch domain (321 to 609 residues) expressed in Escherichia coli DE3 cells incubated for 30 mins by fluorescence polarization assay	B	9.85	pIC50	0.14	nM	IC50	J Med Chem (2020) 63: 11149-11168 [PMID:32902980]
ChEMBL	Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) assessed as thermal stabilization by sypro orange dye based thermal shift assay	B	4.89	pEC50	13000	nM	EC50	J Med Chem (2019) 62: 8028-8052 [PMID:31411465]
kelch like ECH-associated protein 1/Kelch-like ECH-associated protein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3562164] [GtoPdb: 2757] [UniProtKB: Q9Z2X8]
ChEMBL	Binding affinity to mouse Keap1 Kelch domain expressed in Escherichia coli BL21 by VP-ITC assay	B	5.22	pKd	6000	nM	Kd	J Med Chem (2016) 59: 10837-10858 [PMID:27690435]

ChEMBL data shown on this page come from version 34:

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]