ChEMBL ligand: CHEMBL279107 (1,4,5-InsP3, Ionositol 1,4,5-Triphosphate)
Inositol 1,4,5-trisphosphate binding protein in Rat [ChEMBL: CHEMBL3364] [UniProtKB: Q62688] There should be some charts here, you may need to enable JavaScript!
IP3R1/Inositol 1,4,5-trisphosphate receptor type 1 in Human [ChEMBL: CHEMBL4046] [GtoPdb: 743] [UniProtKB: Q14643] 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!
IP3R3/Inositol 1,4,5-trisphosphate receptor type 3 in Human [ChEMBL: CHEMBL3904] [GtoPdb: 745] [UniProtKB: Q14573] Inositol 1,4,5-trisphosphate receptor type 3 in Bovine [ChEMBL: CHEMBL2853] [UniProtKB: Q8WN95] There should be some charts here, you may need to enable JavaScript!
IP3 kinase A/Inositol-trisphosphate 3-kinase A in Rat [ChEMBL: CHEMBL3261] [GtoPdb: 1447] [UniProtKB: P17105] There should be some charts here, you may need to enable JavaScript!
Type 1 InsP3 receptor isoform S2 in Pig [ChEMBL: CHEMBL2950] [UniProtKB: P79248] There should be some charts here, you may need to enable JavaScript!
INPP5A/Type I inositol-1,4,5-trisphosphate 5-phosphatase in Human [ChEMBL: CHEMBL4243] [GtoPdb: 1453] [UniProtKB: Q14642] 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
Inositol 1,4,5-trisphosphate binding protein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3364] [UniProtKB: Q62688]
ChEMBL	Compound was tested for inhibition of specific [3H]Ins(1,4,5)P3 binding to Inositol 1,4,5-trisphosphate receptor in rat cerebellar membranes.	B	6.82	pIC50	150	nM	IC50	Bioorg Med Chem Lett (1996) 6: 2197-2200
ChEMBL	Compound was tested for inhibition of specific [3H]Ins(1,4,5)P3 binding to Inositol 1,4,5-trisphosphate receptor in rat cerebellar membranes.	B	7.4	pIC50	40	nM	IC50	Bioorg Med Chem Lett (1996) 6: 2197-2200
IP3R1/Inositol 1,4,5-trisphosphate receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4046] [GtoPdb: 743] [UniProtKB: Q14643]
ChEMBL	Dissociation constant using IP3-binding domain (IBD) of human Type 1 inositol 1,4,5-trisphosphate receptor	B	6.59	pKd	260	nM	Kd	Bioorg Med Chem Lett (2002) 12: 911-913 [PMID:11958992]
ChEMBL	Binding affinity against Ins(1,4,5)P3 receptor in swiss 3T3 cells	B	6.52	pIC50	300	nM	IC50	Bioorg Med Chem Lett (1995) 5: 1225-1230
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]-InsP3 from rat type-1 InsP3 receptor expressed in sf9 cell membranes in cytosol like medium containing Mg-ATP	B	6.89	pKd	128.82	nM	Kd	Medchemcomm (2018) 9: 1105-1113 [PMID:30079174]
ChEMBL	Displacement of [3H]-InsP3 from rat type-1 InsP3 receptor expressed in sf9 cell membranes in cytosol like medium containing Mg-ATP	B	6.89	pKd	128	nM	Kd	Medchemcomm (2018) 9: 1105-1113 [PMID:30079174]
ChEMBL	Displacement of [3H]IP3 from full-length rat recombinant IP3R1 expressed in chicken DT40 cells by equilibrium competitive binding assay	B	7.9	pKd	12.5	nM	Kd	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Displacement of [3H]IP3 from rat IP3R1 expressed in human HEK cells assessed as dissociation constant by radioligand binding assay	B	8.06	pKd	8.71	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	8.06	pKd	8.71	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	8.06	pKd	8.7	nM	Kd	J Med Chem (2020) 63: 5442-5457 [PMID:32286062]
ChEMBL	Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) K52E mutant expressed in chicken DT40 cells by equilibrium competitive binding assay	B	8.58	pKd	2.64	nM	Kd	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Displacement of [3H]IP3 from rat recombinant N-terminal IP3R1 (1-604) expressed in chicken DT40 cells by equilibrium competitive binding assay	B	8.63	pKd	2.32	nM	Kd	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) D34K mutant expressed in chicken DT40 cells by equilibrium competitive binding assay	B	9.01	pKd	0.98	nM	Kd	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) R36E mutant expressed in chicken DT40 cells by equilibrium competitive binding assay	B	9.34	pKd	0.46	nM	Kd	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) K127E mutant expressed in chicken DT40 cells by equilibrium competitive binding assay	B	9.35	pKd	0.45	nM	Kd	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) V33K mutant expressed in chicken DT40 cells by equilibrium competitive binding assay	B	9.57	pKd	0.27	nM	Kd	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Displacement of [3H]IP3 from rat recombinant IP3R1 binding core residue (224-604) expressed in chicken DT40 cells by equilibrium competitive binding assay	B	9.68	pKd	0.21	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	6.68	pEC50	209	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	6.68	pEC50	208.93	nM	EC50	J Med Chem (2020) 63: 3238-3251 [PMID:32052631]
ChEMBL	Agonist activity at rat IP3R1 expressed in DT40 cells assessed as increase in calcium release by Mag-fluo4 dye based assay	B	6.88	pEC50	133	nM	EC50	J Med Chem (2020) 63: 3238-3251 [PMID:32052631]
ChEMBL	Agonist activity at rat IP3R1 expressed in DT40 cells assessed as increase in calcium release by Mag-fluo4 dye based assay	B	6.88	pEC50	131.83	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	6.9	pEC50	126	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	6.9	pEC50	125.89	nM	EC50	J Med Chem (2020) 63: 5442-5457 [PMID:32286062]
ChEMBL	Agonist activity at rat recombinant IP3R1 K52E mutant expressed in chicken DT40 cells assessed as calcium release from intracellular stores	F	7.07	pEC50	85	nM	EC50	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Agonist activity at rat type-1 InsP3 receptor expressed in chicken DT40 cells in cytosol like medium assessed as increase in calcium release by fluorescence assay	B	7.21	pEC50	62	nM	EC50	Medchemcomm (2018) 9: 1105-1113 [PMID:30079174]
ChEMBL	Agonist activity at rat type-1 InsP3 receptor expressed in chicken DT40 cells in cytosol like medium assessed as increase in calcium release by fluorescence assay	B	7.21	pEC50	61.66	nM	EC50	Medchemcomm (2018) 9: 1105-1113 [PMID:30079174]
ChEMBL	Agonist activity at rat recombinant IP3R1 R36E mutant expressed in chicken DT40 cells assessed as calcium release from intracellular stores	F	7.39	pEC50	40.8	nM	EC50	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Agonist activity at rat recombinant IP3R1 D34K mutant expressed in chicken DT40 cells assessed as calcium release from intracellular stores	F	7.58	pEC50	26.6	nM	EC50	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Agonistic potency at rat IP3 type 1 receptor expressed in chicken DT40 cells	F	7.61	pEC50	24.8	nM	EC50	J Med Chem (2006) 49: 1900-1909 [PMID:16539376]
ChEMBL	Activity at rat IP3 type 1 receptor expressed in DT40 cell assessed as calcium ion mobilization	F	7.61	pEC50	24.8	nM	EC50	J Med Chem (2006) 49: 5750-5758 [PMID:16970399]
ChEMBL	Agonist activity at rat IP3R1 expressed in chicken DT40 cells assessed as induction of Ca2+ release	F	7.64	pEC50	23	nM	EC50	J Med Chem (2012) 55: 1706-1720 [PMID:22248345]
ChEMBL	Agonist activity at rat recombinant IP3R1 V33K mutant expressed in chicken DT40 cells assessed as calcium release from intracellular stores	F	7.65	pEC50	22.3	nM	EC50	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
ChEMBL	Agonist activity at rat recombinant IP3R1 expressed in chicken DT40 cells assessed as calcium release from intracellular stores	F	7.7	pEC50	20	nM	EC50	Nat Chem Biol (2009) 5: 631-639 [PMID:19668195]
IP3R3/Inositol 1,4,5-trisphosphate receptor type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3904] [GtoPdb: 745] [UniProtKB: Q14573]
ChEMBL	Dissociation constant of compound was measured in IP3-binding domain(IBD) of human Inositol 1,4,5-trisphosphate receptor at pH 7.4	B	6.71	pKd	195	nM	Kd	Bioorg Med Chem Lett (1999) 9: 1697-1702 [PMID:10397504]
Inositol 1,4,5-trisphosphate receptor type 3 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2853] [UniProtKB: Q8WN95]
ChEMBL	Binding affinity against Inositol 1,4,5-trisphosphate receptor on bovine adrenal cortex microsomes.	B	4.85	pIC50	14000	nM	IC50	J Med Chem (1999) 42: 4824-4835 [PMID:10579845]
IP3 kinase A/Inositol-trisphosphate 3-kinase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3261] [GtoPdb: 1447] [UniProtKB: P17105]
ChEMBL	Binding affinity against recombinant plasmid rat brain IP3K by overexpressing in Escherichia coli	B	4.36	pIC50	43700	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2981-2984 [PMID:12941316]
ChEMBL	Binding affinity against recombinant plasmid rat brain IP3K by overexpressing in Escherichia coli	B	5.2	pIC50	6300	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2981-2984 [PMID:12941316]
ChEMBL	Binding affinity against recombinant plasmid rat brain IP3K by overexpressing in Escherichia coli	B	5.59	pIC50	2600	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2981-2984 [PMID:12941316]
Type 1 InsP3 receptor isoform S2 in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2950] [UniProtKB: P79248]
ChEMBL	Binding affinity of compound was determined by its ability to displace specifically bound Inositol 1,4,5-trisphosphate receptor from purified porcine cerebellum membrane	B	7.7	pIC50	20	nM	IC50	Bioorg Med Chem Lett (1995) 5: 831-834
INPP5A/Type I inositol-1,4,5-trisphosphate 5-phosphatase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4243] [GtoPdb: 1453] [UniProtKB: Q14642]
ChEMBL	Tested for inhibition of 5-phosphatase isolated from human erythrocyte membrane (S substrate)	B	4.82	pKi	15000	nM	Ki	J Med Chem (1993) 36: 3035-3038 [PMID:8411022]

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]