ChEMBL ligand: CHEMBL204385
IP3R1/Inositol 1,4,5-trisphosphate receptor type 1 in Rat [ChEMBL: CHEMBL2804] [GtoPdb: 743] [UniProtKB: P29994] 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
IP3R1/Inositol 1,4,5-trisphosphate receptor type 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2804] [GtoPdb: 743] [UniProtKB: P29994]
ChEMBL	Displacement of [3H]IP3 from rat IP3R1 expressed in human HEK cells assessed as dissociation constant by radioligand binding assay	B	8.12	pKd	7.59	nM	Kd	J Med Chem (2020) 63: 3238-3251 [PMID:32052631]
ChEMBL	Displacement of [3H]IP3 from rat IP3R1 expressed in human HEK cells assessed as dissociation constant by radioligand binding assay	B	8.12	pKd	7.59	nM	Kd	J Med Chem (2020) 63: 3238-3251 [PMID:32052631]
ChEMBL	Displacement of [3H]-IP3 from IP3R1 in Wistar rat cerebellar membrane measured after 5 mins by liquid scintillation counting method	B	8.85	pKd	1.4	nM	Kd	J Med Chem (2020) 63: 5442-5457 [PMID:32286062]
ChEMBL	Displacement of [3H]IP3 from full-length rat recombinant IP3R1 expressed in chicken DT40 cells by equilibrium competitive binding assay	B	8.9	pKd	1.26	nM	Kd	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Agonist activity at rat IP3R1 expressed in human HEK cells assessed as increase in calcium release by Mag-fluo4 dye based assay	B	6.81	pEC50	155	nM	EC50	J Med Chem (2020) 63: 3238-3251 [PMID:32052631]
ChEMBL	Agonist activity at rat IP3R1 expressed in human HEK cells assessed as increase in calcium release by Mag-fluo4 dye based assay	B	6.81	pEC50	154.88	nM	EC50	J Med Chem (2020) 63: 3238-3251 [PMID:32052631]
ChEMBL	Agonist activity at rat IP3R1 expressed in HEK cells assessed as increase in calcium release in cytosol by measuring fluorescence signal by Mag-Fluo4 dye based assay	B	7.62	pEC50	24	nM	EC50	J Med Chem (2020) 63: 5442-5457 [PMID:32286062]
ChEMBL	Agonist activity at rat IP3R1 expressed in HEK cells assessed as increase in calcium release in cytosol by measuring fluorescence signal by Mag-Fluo4 dye based assay	B	7.62	pEC50	23.99	nM	EC50	J Med Chem (2020) 63: 5442-5457 [PMID:32286062]
ChEMBL	Agonist activity at rat IP3R1 expressed in chicken DT40 cells assessed as induction of Ca2+ release	F	8.55	pEC50	2.8	nM	EC50	J Med Chem (2012) 55: 1706-1720 [PMID:22248345]
ChEMBL	Activity at rat IP3 type 1 receptor expressed in DT40 cell assessed as calcium ion mobilization	F	8.68	pEC50	2.1	nM	EC50	J Med Chem (2006) 49: 5750-5758 [PMID:16970399]
ChEMBL	Agonistic potency at rat IP3 type 1 receptor expressed in chicken DT40 cells	F	8.68	pEC50	2.1	nM	EC50	J Med Chem (2006) 49: 1900-1909 [PMID:16539376]
ChEMBL	Agonist activity at rat recombinant IP3R1 expressed in chicken DT40 cells assessed as calcium release from intracellular stores	F	8.82	pEC50	1.5	nM	EC50	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]

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]