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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]