Protein Information

General Information of the Protein

Protein ID	PT05788
Protein Name	Inositol 1,4,5-trisphosphate receptor type 1
Secondarily Protein Name	IP3 receptor isoform 1 Type 1 inositol 1,4,5-trisphosphate receptor
Gene Name	ITPR1
Secondarily Gene Name	Insp3r
Sequence	MSDKMSSFLHIGDICSLYAEGSTNGFISTLGLVDDRCVVQPEAGDLNNPPKKFRDCLFKLCPMNRYSAQKQFWKAAKPGANSTTDAVLLNKLHHAADLEKKQNETENRKLLGTVIQYGNVIQLLHLKSNKYLTVNKRLPALLEKNAMRVTLDEAGNEGSWFYIQPFYKLRSIGDSVVIGDKVVLNPVNAGQPLHASSHQLVDNPGCNEVNSVNCNTSWKIVLFMKWSDNKDDILKGGDVVRLFHAEQEKFLTCDEHRKKQHVFLRTTGRQSATSATSSKALWEVEVVQHDPCRGGAGYWNSLFRFKHLATGHYLAAEVDPDFEEECLEFQPSVDPDQDASRSRLRNAQEKMVYSLVSVPEGNDISSIFELDPTTLRGGDSLVPRNSYVRLRHLCTNTWVHSTNIPIDKEEEKPVMLKIGTSPLKEDKEAFAIVPVSPAEVRDLDFANDASKVLGSIAGKLEKGTITQNERRSVTKLLEDLVYFVTGGTNSGQDVLEVVFSKPNRERQKLMREQNILKQIFKLLQAPFTDCGDGPMLRLEELGDQRHAPFRHICRLCYRVLRHSQQDYRKNQEYIAKQFGFMQKQIGYDVLAEDTITALLHNNRKLLEKHITAAEIDTFVSLVRKNREPRFLDYLSDLCVSMNKSIPVTQELICKAVLNPTNADILIETKLVLSRFEFEGVSTGENALEAGEDEEEVWLFWRDSNKEIRSKSVRELAQDAKEGQKEDRDVLSYYRYQLNLFARMCLDRQYLAINEISGQLDVDLILRCMSDENLPYDLRASFCRLMLHMHVDRDPQEQVTPVKYARLWSEIPSEIAIDDYDSSGASKDEIKERFAQTMEFVEEYLRDVVCQRFPFSDKEKNKLTFEVVNLARNLIYFGFYNFSDLLRLTKILLAILDCVHVTTIFPISKMTKGEENKGSNVMRSIHGVGELMTQVVLRGGGFLPMTPMAAAPEGNVKQAEPEKEDIMVMDTKLKIIEILQFILNVRLDYRISCLLCIFKREFDESNSQSSETSSGNSSQEGPSNVPGALDFEHIEEQAEGIFGGSEENTPLDLDDHGGRTFLRVLLHLTMHDYPPLVSGALQLLFRHFSQRQEVLQAFKQVQLLVTSQDVDNYKQIKQDLDQLRSIVEKSELWVYKGQGPDEPMDGASGENEHKKTEEGTSKPLKHESTSSYNYRVVKEILIRLSKLCVQESASVRKSRKQQQRLLRNMGAHAVVLELLQIPYEKAEDTKMQEIMRLAHEFLQNFCAGNQQNQALLHKHINLFLNPGILEAVTMQHIFMNNFQLCSEINERVVQHFVHCIETHGRNVQYIKFLQTIVKAEGKFIKKCQDMVMAELVNSGEDVLVFYNDRASFQTLIQMMRSERDRMDENSPLFMYHIHLVELLAVCTEGKNVYTEIKCNSLLPLDDIVRVVTHEDCIPEVKIAYINFLNHCYVDTEVEMKEIYTSNHMWKLFENFLVDICRACNNTSDRKHADSVLEKYVTEIVMSIVTTFFSSPFSDQSTTLQTRQPVFVQLLQGVFRVYHCNWLMPSQKASVESCIRVLSDVAKSRAIAIPVDLDSQVNNLFLKSHNIVQKTAMNWRLSARNAARRDSVLAASRDYRNIIERLQDIVSALEDRLRPLVQAELSVLVDVLHRPELLFPENTDARRKCESGGFICKLIKHTKQLLEENEEKLCIKVLQTLREMMTKDRGYGEKQISIDELENAELPQPPEAENSTEQELEPSPPLRQLEDHKRGEALRQILVNRYYGNIRPSGRRESLTSFGNGPLSPGGPSKPGGGGGGPGSGSTSRGEMSLAEVQCHLDKEGASNLVIDLIMNASSDRVFHESILLAIALLEGGNTTIQHSFFCRLTEDKKSEKFFKVFYDRMKVAQQEIKATVTVNTSDLGNKKKDDEVDRDAPSRKKAKEPTTQITEEVRDQLLEASAATRKAFTTFRREADPDDHYQSGEGTQATTDKAKDDLEMSAVITIMQPILRFLQLLCENHNRDLQNFLRCQNNKTNYNLVCETLQFLDCICGSTTGGLGLLGLYINEKNVALINQTLESLTEYCQGPCHENQNCIATHESNGIDIITALILNDINPLGKKRMDLVLELKNNASKLLLAIMESRHDSENAERILYNMRPKELVEVIKKAYMQGEVEFEDGENGEDGAASPRNVGHNIYILAHQLARHNKELQTMLKPGGQVDGDEALEFYAKHTAQIEIVRLDRTMEQIVFPVPSICEFLTKESKLRIYYTTERDEQGSKINDFFLRSEDLFNEMNWQKKLRAQPVLYWCARNMSFWSSISFNLAVLMNLLVAFFYPFKGVRGGTLEPHWSGLLWTAMLISLAIVIALPKPHGIRALIASTILRLIFSVGLQPTLFLLGAFNVCNKIIFLMSFVGNCGTFTRGYRAMVLDVEFLYHLLYLLICAMGLFVHEFFYSLLLFDLVYREETLLNVIKSVTRNGRPIILTAALALILVYLFSIVGYLFFKDDFILEVDRLPNETAGPETGESLANDFLYSDVCRVETGENCTSPAPKEELLPVEETEQDKEHTCETLLMCIVTVLSHGLRSGGGVGDVLRKPSKEEPLFAARVIYDLLFFFMVIIIVLNLIFGVIIDTFADLRSEKQKKEEILKTTCFICGLERDKFDNKTVTFEEHIKEEHNMWHYLCFIVLVKVKDSTEYTGPESYVAEMIRERNLDWFPRMRAMSLVSSDSEGEQNELRNLQEKLESTMKLVTNLSGQLSELKDQMTEQRKQKQRIGLLGHPPHMNVNPQQPA Show/Hide
Organism	Rattus norvegicus, Rat
Protein Classification	Ion channel > Ligand-gated ion channel > IP3 receptor
Function	Intracellular channel that mediates calcium release from the endoplasmic reticulum following stimulation by inositol 1,4,5-trisphosphate. Involved in the regulation of epithelial secretion of electrolytes and fluid through the interaction with AHCYL1 Plays a role in ER stress-induced apoptosis. Cytoplasmic calcium released from the ER triggers apoptosis by the activation of CaM kinase II, eventually leading to the activation of downstream apoptosis pathways. Show/Hide
Uniprot ID	Primary ID: P29994 Secondarily ID: Q62869 Show/Hide
Ensembl ID	ENSG00000150995
Subcellular Location	Endoplasmic reticulum membrane Cytoplasmic vesicle Secretory vesicle membrane Cytoplasm Perinuclear region

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000302 , DT40

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0376247 Compound Info	2-[5-(6-amino-9H-9-purinyl)-2-hydroxymethyl-4-oxyphosphate-(2R,3R,4R,5R)-tetrahydro-3-furanyloxy]-6-hydroxymethyl-4,5-dioxyphosphate-(2R,3R,4S,5R,6R)-tetrahydro-2H-3-pyranol Show/Hide	C16H26N5O18P3	4
1	EC50 = 1.5 nM Bioactivity Info	TI LI LO TS
2	EC50 = 2.1 nM Bioactivity Info	TI LI LO TS
3	EC50 = 2.8 nM Bioactivity Info	TI LI LO TS
4	Kd = 1.26 nM Bioactivity Info	TI LI LO TS
CP0856060 Compound Info	5'-Deoxy-5'-phenyladenophostin A Show/Hide	C22H30N5O17P3	1
1	EC50 = 2.1 nM Bioactivity Info	TI LI LO TS
CP0846817 Compound Info	5'-deoxy-5'-phenethyladenophostin A 2',3'',4''-trisphosphate Show/Hide	C24H34N5O17P3	1
1	EC50 = 2.7 nM Bioactivity Info	TI LI LO TS
CP0372443 Compound Info	[(1R,2R,3S,4R,5S,6R)-4-[2-[2-[(1R,2S,3R,4R,5S,6S)-2,5-dihydroxy-3,4,6-triphosphonooxycyclohexyl]oxyethylcarbamoylamino]ethoxy]-2,5-dihydroxy-3,6-diphosphonooxycyclohexyl]oxy-trihydroxyphosphanium Show/Hide	C17H40N2O31P6	13
1	EC50 = 2.7 nM Bioactivity Info	TI LI LO TS
2	EC50 = 7.7 nM Bioactivity Info	TI LI LO TS
3	EC50 = 11.5 nM Bioactivity Info	TI LI LO TS
4	EC50 = 15.8 nM Bioactivity Info	TI LI LO TS
5	EC50 = 19.5 nM Bioactivity Info	TI LI LO TS
6	Kd = 0.18 nM Bioactivity Info	TI LI LO TS
7	Kd = 0.27 nM Bioactivity Info	TI LI LO TS
8	Kd = 0.32 nM Bioactivity Info	TI LI LO TS
9	Kd = 0.4 nM Bioactivity Info	TI LI LO TS
10	Kd = 0.41 nM Bioactivity Info	TI LI LO TS
11	Kd = 0.45 nM Bioactivity Info	TI LI LO TS
12	Kd = 0.68 nM Bioactivity Info	TI LI LO TS
13	Kd = 0.78 nM Bioactivity Info	TI LI LO TS
CP0869652 Compound Info	5'-deoxy-5'-benzyladenophostin A 2',3'',4''-trisphosphate Show/Hide	C23H32N5O17P3	1
1	EC50 = 2.8 nM Bioactivity Info	TI LI LO TS
CP0456843 Compound Info	[(2R,3R,4R,5S)-2-(6-aminopurin-9-yl)-4-[[(2R,3S,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-diphosphonooxyoxan-2-yl]methyl]-5-(hydroxymethyl)oxolan-3-yl] dihydrogen phosphate Show/Hide	C17H28N5O17P3	1
1	EC50 = 4 nM Bioactivity Info	TI LI LO TS
CP0382474 Compound Info	[(2R,3R,4R,5R)-2-(2,4-dioxopyrimidin-1-yl)-4-[(2R,3R,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-diphosphonooxyoxan-2-yl]oxy-5-(hydroxymethyl)oxolan-3-yl] dihydrogen phosphate Show/Hide	C15H25N2O20P3	1
1	EC50 = 4.6 nM Bioactivity Info	TI LI LO TS
CP0493011 Compound Info	[(1R,2R,3S,4R,5S,6R)-4-[2-[2-[2-[2-[2-[2-[2-[2-[(1R,2S,3R,4R,5S,6S)-2,5-dihydroxy-3,4,6-triphosphonooxycyclohexyl]oxyethylcarbamoyloxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxycarbonylamino]ethoxy]-2,5-dihydroxy-3,6-diphosphonooxycyclohexyl]oxy-trihydroxyphosphanium Show/Hide	C30H64N2O39P6	4
1	EC50 = 4.9 nM Bioactivity Info	TI LI LO TS
2	Kd = 0.18 nM Bioactivity Info	TI LI LO TS
3	Kd = 0.47 nM Bioactivity Info	TI LI LO TS
4	Kd = 0.86 nM Bioactivity Info	TI LI LO TS
CP0373519 Compound Info	CHEMBL1212943 Show/Hide	C17H40N2O31P6	4
1	EC50 = 5 nM Bioactivity Info	TI LI LO TS
2	Kd = 0.14 nM Bioactivity Info	TI LI LO TS
3	Kd = 0.42 nM Bioactivity Info	TI LI LO TS
4	Kd = 0.9 nM Bioactivity Info	TI LI LO TS
CP0373522 Compound Info	CHEMBL1213160 Show/Hide	C17H42N2O37P8	4
1	EC50 = 5 nM Bioactivity Info	TI LI LO TS
2	Kd = 0.2 nM Bioactivity Info	TI LI LO TS
3	Kd = 0.36 nM Bioactivity Info	TI LI LO TS
4	Kd = 0.89 nM Bioactivity Info	TI LI LO TS
CP0529794 Compound Info	[(2R,3R,4R,5S)-2-(2,4-dioxopyrimidin-1-yl)-4-[[(2R,3S,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-diphosphonooxyoxan-2-yl]methyl]-5-(hydroxymethyl)oxolan-3-yl] dihydrogen phosphate Show/Hide	C16H27N2O19P3	1
1	EC50 = 11.3 nM Bioactivity Info	TI LI LO TS
CP0194242 Compound Info	1,4,5-Insp3 Show/Hide	C6H15O15P3	15
1	EC50 = 20 nM Bioactivity Info	TI LI LO TS
2	EC50 = 22.3 nM Bioactivity Info	TI LI LO TS
3	EC50 = 23 nM Bioactivity Info	TI LI LO TS
4	EC50 = 24.8 nM Bioactivity Info	TI LI LO TS
5	EC50 = 26.6 nM Bioactivity Info	TI LI LO TS
6	EC50 = 40.8 nM Bioactivity Info	TI LI LO TS
7	EC50 = 85 nM Bioactivity Info	TI LI LO TS
8	Kd = 0.21 nM Bioactivity Info	TI LI LO TS
9	Kd = 0.27 nM Bioactivity Info	TI LI LO TS
10	Kd = 0.45 nM Bioactivity Info	TI LI LO TS
11	Kd = 0.46 nM Bioactivity Info	TI LI LO TS
12	Kd = 0.98 nM Bioactivity Info	TI LI LO TS
13	Kd = 2.32 nM Bioactivity Info	TI LI LO TS
14	Kd = 2.64 nM Bioactivity Info	TI LI LO TS
15	Kd = 12.5 nM Bioactivity Info	TI LI LO TS
CP0488638 Compound Info	[(1R,2S,3R,4S,5S,6R)-2,5-dihydroxy-3-[2-[2-[(2S,3R,5S,6R)-2,3,4,5,6-pentahydroxycyclohexyl]oxyethylcarbamoylamino]ethoxy]-4,6-diphosphonooxycyclohexyl] dihydrogen phosphate Show/Hide	C17H35N2O22P3	4
1	EC50 = 21 nM Bioactivity Info	TI LI LO TS
2	Kd = 0.33 nM Bioactivity Info	TI LI LO TS
3	Kd = 2.81 nM Bioactivity Info	TI LI LO TS
4	Kd = 7.82 nM Bioactivity Info	TI LI LO TS
CP0373520 Compound Info	[(1S,2R,3S,4R,5R,6S)-2-[2-(adamantane-1-carbonylamino)ethoxy]-3,6-dihydroxy-4,5-diphosphonooxycyclohexyl] dihydrogen phosphate Show/Hide	C19H34NO16P3	4
1	EC50 = 30 nM Bioactivity Info	TI LI LO TS
2	Kd = 0.2 nM Bioactivity Info	TI LI LO TS
3	Kd = 1.63 nM Bioactivity Info	TI LI LO TS
4	Kd = 7.62 nM Bioactivity Info	TI LI LO TS
CP0470760 Compound Info	(1R,2R,3S,4R,6S)-3,6-dihydroxycyclohexane-1,2,4-triyl triphosphate Show/Hide	C6H15O14P3	4
1	EC50 = 32 nM Bioactivity Info	TI LI LO TS
2	Kd = 0.22 nM Bioactivity Info	TI LI LO TS
3	Kd = 4.01 nM Bioactivity Info	TI LI LO TS
4	Kd = 17.1 nM Bioactivity Info	TI LI LO TS
CP0470762 Compound Info	(1R,2R,3S,4S,5R,6S)-5-(2-aminoethoxy)-3,6-dihydroxycyclohexane-1,2,4-triyl triphosphate Show/Hide	C8H20NO15P3	4
1	EC50 = 42 nM Bioactivity Info	TI LI LO TS
2	Kd = 0.52 nM Bioactivity Info	TI LI LO TS
3	Kd = 13.5 nM Bioactivity Info	TI LI LO TS
4	Kd = 43.6 nM Bioactivity Info	TI LI LO TS
CP0529793 Compound Info	2-[(2R,3S,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-diphosphonooxyoxan-2-yl]ethyl dihydrogen phosphate Show/Hide	C8H19O15P3	1
1	EC50 = 49.2 nM Bioactivity Info	TI LI LO TS
CP0846818 Compound Info	(3S,4R,5R)-5-benzyl-4-{[(2R,3R,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-bis(phosphonatooxy)oxan-2-yl]oxy}oxolan-3-yl phosphate Show/Hide	C17H27O17P3	1
1	EC50 = 53.3 nM Bioactivity Info	TI LI LO TS
CP0432911 Compound Info	[(2R,3R,4R,5R,6R)-2-[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl]oxy-3-hydroxy-6-(hydroxymethyl)-5-phosphonooxyoxan-4-yl] dihydrogen phosphate Show/Hide	C16H25N5O15P2	1
1	EC50 = 107 nM Bioactivity Info	TI LI LO TS
CP0510263 Compound Info	3-[(2R,3S,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-diphosphonooxyoxan-2-yl]propyl dihydrogen phosphate Show/Hide	C9H21O15P3	1
1	EC50 = 213 nM Bioactivity Info	TI LI LO TS
CP0424884 Compound Info	[(2R,3S,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-diphosphonooxyoxan-2-yl]methyl dihydrogen phosphate Show/Hide	C7H17O15P3	1
1	EC50 = 394 nM Bioactivity Info	TI LI LO TS
CP0538062 Compound Info	[(2S,3S,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-diphosphonooxyoxan-2-yl]methyl dihydrogen phosphate Show/Hide	C7H17O15P3	1
1	EC50 = 1080 nM Bioactivity Info	TI LI LO TS
CP0536559 Compound Info	2-[(2S,3S,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-diphosphonooxyoxan-2-yl]ethyl dihydrogen phosphate Show/Hide	C8H19O15P3	1
1	EC50 = 2040 nM Bioactivity Info	TI LI LO TS
CP0424882 Compound Info	3-[(2S,3S,4R,5R,6R)-3-hydroxy-6-(hydroxymethyl)-4,5-diphosphonooxyoxan-2-yl]propyl dihydrogen phosphate Show/Hide	C9H21O15P3	1
1	EC50 = 4430 nM Bioactivity Info	TI LI LO TS
CP0406198 Compound Info	1D-myo-inositol 4,5-bis(dihydrogen phosphate) Show/Hide	C6H14O12P2	1
1	EC50 = 8634 nM Bioactivity Info	TI LI LO TS
CP0521869 Compound Info	[(2R,3R,4R,5R)-5,6-dihydroxy-2-(hydroxymethyl)-4-phosphonooxyoxan-3-yl] dihydrogen phosphate Show/Hide	C6H14O12P2	1
1	EC50 = 25190 nM Bioactivity Info	TI LI LO TS
CP0487241 Compound Info	[(2R,3R,4R,5R)-2-(6-aminopurin-9-yl)-4-[(2R,3R,4R,5S,6R)-3,4-dihydroxy-6-(hydroxymethyl)-5-phosphonooxyoxan-2-yl]oxy-5-(hydroxymethyl)oxolan-3-yl] dihydrogen phosphate Show/Hide	C16H25N5O15P2	1
1	EC50 = 53030 nM Bioactivity Info	TI LI LO TS

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han