ChEMBL ligand: CHEMBL4434776
stimulator of interferon response cGAMP interactor 1/Stimulator of interferon genes protein in Human [ChEMBL: CHEMBL4523377] [GtoPdb: 2902] [UniProtKB: Q86WV6] stimulator of interferon response cGAMP interactor 1/Stimulator of interferon genes protein in Mouse [ChEMBL: CHEMBL4523311] [GtoPdb: 2902] [UniProtKB: Q3TBT3] 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
stimulator of interferon response cGAMP interactor 1/Stimulator of interferon genes protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523377] [GtoPdb: 2902] [UniProtKB: Q86WV6]
ChEMBL	Binding affinity to N-terminal His-tagged wild type human STING CTD (139 to 37 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant by NMR analysis	B	4.74	pKd	18000	nM	Kd	J Med Chem (2024) 67: 1701-1733 [PMID:38290426]
ChEMBL	Displacement of [3H]-cGAMP from full-length wild type human STING by filtration binding assay	B	5.76	pIC50	1720	nM	IC50	J Med Chem (2023) 66: 5584-5610 [PMID:37027512]
ChEMBL	Agonist activity at human STING in STING knockout human THP1-Blue ISG cells incubated for 24 hrs in presence of PMA by luciferase reporter assay	B	4	pEC50	>100000	nM	EC50	J Med Chem (2023) 66: 3327-3347 [PMID:36808996]
ChEMBL	Agonist activity at wild type human STING expressed in baculovirus infected Sf21 insect cells	B	4.62	pEC50	24000	nM	EC50	J Med Chem (2021) 64: 1649-1669 [PMID:33470814]
ChEMBL	Agonist activity at human STING HAQ expressed in baculovirus infected Sf21 insect cells	B	5.08	pEC50	8300	nM	EC50	J Med Chem (2021) 64: 1649-1669 [PMID:33470814]
ChEMBL	Agonist activity at human STING HAQ mutant	B	5.08	pEC50	8300	nM	EC50	Eur J Med Chem (2022) 238: 114482-114482 [PMID:35671593]
ChEMBL	Agonist activity at STING in human THP1-Dual cells assessed as ISG pathway activation incubated for 24 hrs by Quanti-Luc or Quanti-blue reagent based luminescence assay	B	5.09	pEC50	8140	nM	EC50	Eur J Med Chem (2022) 241: 114627-114627 [PMID:35963129]
ChEMBL	Agonist activity at human STING in human THP1-Blue ISG cells incubated for 24 hrs in presence of PMA by luciferase reporter assay	B	5.45	pEC50	3510	nM	EC50	J Med Chem (2023) 66: 3327-3347 [PMID:36808996]
ChEMBL	STING Biochemical [3H]cGAMP Competition Assay: The individual compounds described in the Examples herein are defined as STING agonists by (i) binding to the STING protein as evidenced by a reduction in binding of tritiated cGAMP ligand to the STING protein by at least 20% at 20 uM (concentration of compound being tested) in a STING Biochemical 13H1-cGAMP Competition Assay and (ii) demonstrating interferon production with a 6% or greater induction of IFN-β secretion at 30 uM in the THP1 cell assay (where induction caused by cGAMP at 30 uM was set at 100%).The ability of compounds to bind STING is quantified by the ability to compete with tritiated cGAMP ligand for human STING receptor membrane using a radioactive filter-binding assay. The binding assay employs STING receptor obtained from Hi-Five cell membranes overexpressing full-length HAQ STING prepared in-house and tritiated cGAMP ligand also purified in-house.	B	5.61	pEC50	2480	nM	EC50	US-10730849-B2. Benzo[b]thiophene compounds as STING agonists (2020)
GtoPdb	Determined in a filtration binding assay measuring displacement of [3H]-cGAMP from full length wild type STING.	-	5.61	pEC50	2480	nM	EC50	WO2018067423A1. BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS (2018)
GtoPdb	Determined in a filtration binding assay measuring displacement of [3H]-cGAMP from full length STING (with HAQ modification) in human THP1 cells.	-	5.76	pEC50	1720	nM	EC50	J Med Chem (2020) 63: 3785-3816 [PMID:31820978]; WO2018067423A1. BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS (2018)
ChEMBL	Binding affinity to STING HAQ variant (unknown origin)	B	5.76	pEC50	1720	nM	EC50	Eur J Med Chem (2022) 241: 114627-114627 [PMID:35963129]
ChEMBL	STING Biochemical [3H]cGAMP Competition Assay: The individual compounds described in the Examples herein are defined as STING agonists by (i) binding to the STING protein as evidenced by a reduction in binding of tritiated cGAMP ligand to the STING protein by at least 20% at 20 uM (concentration of compound being tested) in a STING Biochemical 13H1-cGAMP Competition Assay and (ii) demonstrating interferon production with a 6% or greater induction of IFN-β secretion at 30 uM in the THP1 cell assay (where induction caused by cGAMP at 30 uM was set at 100%).The ability of compounds to bind STING is quantified by the ability to compete with tritiated cGAMP ligand for human STING receptor membrane using a radioactive filter-binding assay. The binding assay employs STING receptor obtained from Hi-Five cell membranes overexpressing full-length HAQ STING prepared in-house and tritiated cGAMP ligand also purified in-house.	B	5.76	pEC50	1720	nM	EC50	US-10730849-B2. Benzo[b]thiophene compounds as STING agonists (2020)
ChEMBL	Displacement of [3H]-cGAMP from full length STING HAQ mutant in human THP1 cells by filtration binding assay	B	5.76	pEC50	1720	nM	EC50	J Med Chem (2020) 63: 3785-3816 [PMID:31820978]
stimulator of interferon response cGAMP interactor 1/Stimulator of interferon genes protein in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523311] [GtoPdb: 2902] [UniProtKB: Q3TBT3]
ChEMBL	Agonist activity at mouse STING in mouse RAW-Lucia ISG cells incubated for 24 hrs in presence of PMA by luciferase reporter assay	B	4.46	pEC50	34540	nM	EC50	J Med Chem (2023) 66: 3327-3347 [PMID:36808996]

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]