ChEMBL ligand: CHEMBL4297310 (Dordaviprona, Dordaviprone, NSC-350625, Onc 201, Onc-201, Onc201, ONC201, TIC-10, TIC10)
caseinolytic mitochondrial matrix peptidase proteolytic subunit/ATP-dependent Clp protease proteolytic subunit, mitochondrial in Human [ChEMBL: CHEMBL4523305] [GtoPdb: 3273] [UniProtKB: Q16740] There should be some charts here, you may need to enable JavaScript!
GPR132/Probable G-protein coupled receptor 132 in Human [ChEMBL: CHEMBL3085618] [GtoPdb: 128] [UniProtKB: Q9UNW8] 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
caseinolytic mitochondrial matrix peptidase proteolytic subunit/ATP-dependent Clp protease proteolytic subunit, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523305] [GtoPdb: 3273] [UniProtKB: Q16740]
ChEMBL	Binding affinity to human CLpP assessed as dissociation constant by ITC method	B	4.55	pKd	28200	nM	Kd	J Med Chem (2022) 65: 7629-7655 [PMID:35609303]
ChEMBL	Activation of recombinant human CLpP using Ac-WLA-AMC as substrate preincubated for 60 mins followed by substrate addition by fluorescence based assay	B	4.9	pEC50	12500	nM	EC50	RSC Med Chem (2023) 14: 2206-2230 [PMID:37974956]
ChEMBL	Binding affinity to human Casein lysing protease P (HsClpP) assessed as change in melting temperature measured after 2 hrs differential scanning fluorimetry (DSF) assay	B	5.38	pEC50	4130	nM	EC50	J Med Chem (2024) 67: 6769-6792 [PMID:38620134]
ChEMBL	Agonist activity at human Casein lysing protease P (HsClpP) assessed as increase in peptidase activity using fluorescent peptide AC-WLA-AMC as substrate measured after 2 hrs by SDS-PAGE/Kamus brilliant blue assay	B	5.62	pEC50	2400	nM	EC50	J Med Chem (2024) 67: 6769-6792 [PMID:38620134]
ChEMBL	Activation of human recombinant his-sumo tagged ClpP expressed in Escherichia coli BL21 (DE3) using FITC-casein as substrate preincubated for 30 mins followed by substrate addition and measured every 60 secs for 30 mins by fluorescence based microplate reader analysis	B	5.76	pEC50	1720	nM	EC50	J Med Chem (2024) 67: 15328-15352 [PMID:39172943]
ChEMBL	Agonist activity at human Casein lysing protease P (HsClpP) assessed as proteolytic activity by measuring alpha-casein hydrolysis measured after 2 hrs incubation by fluorescence assay	B	5.83	pEC50	1490	nM	EC50	J Med Chem (2024) 67: 6769-6792 [PMID:38620134]
ChEMBL	Agonist activity at human CLpP (57 to 277 amino acids) expressed in Escherichia coli using fluorogenic peptide AC-WLA-AMC as substrate incubated for 10 mins by fluorescence based assay	B	6	pEC50	1000	nM	EC50	J Med Chem (2022) 65: 7629-7655 [PMID:35609303]
ChEMBL	Agonist activity at human ClpP expressed in Escherichia coli using AC-WLA-AMC as substrate measured every 5 mins for 1 hr by fluorescence based analysis	B	7.92	pEC50	12.02	nM	EC50	J Med Chem (2024) 67: 2812-2836 [PMID:38329974]
GPR132/Probable G-protein coupled receptor 132 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3085618] [GtoPdb: 128] [UniProtKB: Q9UNW8]
ChEMBL	Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	F	4.41	pEC50	38600	nM	EC50	J Med Chem (2024) 67: 10567-10588 [PMID:38917049]

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]