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ChEMBL

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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL1981
Target Type SINGLE PROTEIN
Preferred Name Insulin receptor
Synonyms CD_antigen=CD220 | INSR | IR | Insulin receptor subunit alpha | Insulin receptor subunit beta | Insulin receptor
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase insr family

Target Components

Component Description Relationship Accession
Insulin receptor SINGLE PROTEIN P06213

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1201538 INSULIN LISPRO Insulin receptor agonist 4 DailyMed
CHEMBL1201641 INSULIN ZINC SUSP EXTENDED RECOMBINANT HUMAN Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201497 INSULIN GLARGINE Insulin receptor agonist 4 DailyMed
CHEMBL1201627 INSULIN SUSP ISOPHANE SEMISYNTHETIC PURIFIED HUMAN Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201545 INSULIN SUSP ISOPHANE BEEF Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201496 INSULIN ASPART Insulin receptor agonist 4 DailyMed
CHEMBL1201664 INSULIN ASPART PROTAMINE RECOMBINANT Insulin receptor agonist 4 DailyMed
CHEMBL1201611 INSULIN LISPRO PROTAMINE RECOMBINANT Insulin receptor agonist 4 DailyMed
CHEMBL1201629 INSULIN PURIFIED BEEF Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201539 INSULIN PORK Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201656 INSULIN SUSP ISOPHANE PURIFIED PORK Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201638 INSULIN SUSP PROTAMINE ZINC PURIFIED PORK Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201543 INSULIN ZINC SUSP SEMISYNTHETIC PURIFIED HUMAN Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201639 INSULIN ZINC SUSP BEEF Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201631 INSULIN HUMAN Insulin receptor agonist 4 DailyMed DailyMed FDA FDA
CHEMBL1201628 INSULIN SUSP PROTAMINE ZINC BEEF/PORK Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201643 INSULIN ZINC SUSP PROMPT PURIFIED PORK Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201634 INSULIN ZINC SUSP PURIFIED BEEF/PORK Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201635 INSULIN SUSP ISOPHANE BEEF/PORK Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201655 INSULIN SUSP ISOPHANE PURIFIED BEEF Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201542 INSULIN ZINC SUSP EXTENDED PURIFIED BEEF Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201546 INSULIN ZINC SUSP PURIFIED BEEF Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201653 INSULIN ZINC SUSP PURIFIED PORK Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201613 INSULIN GLULISINE Insulin receptor agonist 4 DailyMed
CHEMBL1201630 INSULIN PURIFIED PORK Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201640 INSULIN ZINC SUSP EXTENDED BEEF Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201540 INSULIN SUSP ISOPHANE RECOMBINANT HUMAN Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201541 INSULIN SUSP PROTAMINE ZINC PURIFIED BEEF Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201642 INSULIN ZINC SUSP PROMPT BEEF Insulin receptor agonist 4 DailyMed FDA
CHEMBL1201644 INSULIN ZINC SUSP RECOMBINANT HUMAN Insulin receptor agonist 4 DailyMed FDA
CHEMBL2104391 INSULIN DETEMIR Insulin receptor agonist 4 DailyMed
CHEMBL2107869 INSULIN DEGLUDEC Insulin receptor agonist 4 DailyMed
CHEMBL1091644 LINSITINIB Insulin receptor inhibitor 3 PubMed PubMed PubMed
CHEMBL575448 BMS-754807 Insulin receptor inhibitor 2 PubMed PubMed
CHEMBL3545156 KW-2450 Insulin receptor inhibitor 2 DOI
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000171105
Ensembl ENSG00000171105
GO Cellular Component GO:0005634 (nucleus)
GO:0005768 (endosome)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0005899 (insulin receptor complex)
GO:0005901 (caveola)
GO:0010008 (endosome membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0043231 (intracellular membrane-bounded organelle)
GO:0043235 (receptor complex)
GO:0045202 (synapse)
GO:0070062 (extracellular exosome)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004714 (transmembrane receptor protein tyrosine kinase activity)
GO:0004716 (receptor signaling protein tyrosine kinase activity)
GO:0005009 (insulin-activated receptor activity)
GO:0005159 (insulin-like growth factor receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0005525 (GTP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019901 (protein kinase binding)
GO:0019903 (protein phosphatase binding)
GO:0019904 (protein domain specific binding)
GO:0031405 (lipoic acid binding)
GO:0031994 (insulin-like growth factor I binding)
GO:0031995 (insulin-like growth factor II binding)
GO:0032403 (protein complex binding)
GO:0043423 (3-phosphoinositide-dependent protein kinase binding)
GO:0043548 (phosphatidylinositol 3-kinase binding)
GO:0043559 (insulin binding)
GO:0043560 (insulin receptor substrate binding)
GO:0051425 (PTB domain binding)
GO Biological Process GO:0000187 (activation of MAPK activity)
GO:0001933 (negative regulation of protein phosphorylation)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0003007 (heart morphogenesis)
GO:0005975 (carbohydrate metabolic process)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006468 (protein phosphorylation)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0008284 (positive regulation of cell proliferation)
GO:0008286 (insulin receptor signaling pathway)
GO:0008544 (epidermis development)
GO:0008584 (male gonad development)
GO:0009725 (response to hormone)
GO:0009887 (organ morphogenesis)
GO:0010042 (response to manganese ion)
GO:0010310 (regulation of hydrogen peroxide metabolic process)
GO:0010560 (positive regulation of glycoprotein biosynthetic process)
GO:0010629 (negative regulation of gene expression)
GO:0014823 (response to activity)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0019087 (transformation of host cell by virus)
GO:0023014 (signal transduction by protein phosphorylation)
GO:0030238 (male sex determination)
GO:0030325 (adrenal gland development)
GO:0030335 (positive regulation of cell migration)
GO:0031017 (exocrine pancreas development)
GO:0031667 (response to nutrient levels)
GO:0032147 (activation of protein kinase activity)
GO:0032148 (activation of protein kinase B activity)
GO:0032355 (response to estradiol)
GO:0032410 (negative regulation of transporter activity)
GO:0032868 (response to insulin)
GO:0032869 (cellular response to insulin stimulus)
GO:0033280 (response to vitamin D)
GO:0033574 (response to testosterone)
GO:0034612 (response to tumor necrosis factor)
GO:0038083 (peptidyl-tyrosine autophosphorylation)
GO:0042593 (glucose homeostasis)
GO:0043410 (positive regulation of MAPK cascade)
GO:0045429 (positive regulation of nitric oxide biosynthetic process)
GO:0045444 (fat cell differentiation)
GO:0045471 (response to ethanol)
GO:0045725 (positive regulation of glycogen biosynthetic process)
GO:0045740 (positive regulation of DNA replication)
GO:0045821 (positive regulation of glycolytic process)
GO:0045840 (positive regulation of mitotic nuclear division)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045995 (regulation of embryonic development)
GO:0046326 (positive regulation of glucose import)
GO:0046777 (protein autophosphorylation)
GO:0048639 (positive regulation of developmental growth)
GO:0051290 (protein heterotetramerization)
GO:0051384 (response to glucocorticoid)
GO:0051446 (positive regulation of meiotic cell cycle)
GO:0051897 (positive regulation of protein kinase B signaling)
GO:0060267 (positive regulation of respiratory burst)
GO:0071363 (cellular response to growth factor stimulus)
GO:2000194 (regulation of female gonad development)
Wikipedia Insulin_receptor

Target Cross References - Protein

CGD Hyperinsulinemic hypoglycemia, familial, 5; Rabson-Mendenhall syndrome; Donohoe syndrome
Human Protein Atlas ENSG00000171105
IntAct P06213
Guide to Pharmacology 1800
Open Targets ENSG00000171105
PharmGKB PA202
Pharos P06213 (Tclin)
Reactome R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-74713 (IRS activation.)
R-HSA-74749 (Signal attenuation.)
R-HSA-74751 (Insulin receptor signalling cascade.)
R-HSA-74752 (Signaling by Insulin receptor.)
R-HSA-77387 (Insulin receptor recycling.)
UniProt P06213 Q17RW0 Q59H98 Q9UCB7 Q9UCB8 Q9UCB9

Target Cross References - Domain

InterPro IPR000494 (Rcpt_L-dom.)
IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR002011 (Tyr_kinase_rcpt_2_CS.)
IPR003961 (FN3_dom.)
IPR006211 (Furin-like_Cys-rich_dom.)
IPR006212 (Furin_repeat.)
IPR008266 (Tyr_kinase_AS.)
IPR009030 (Growth_fac_rcpt_.)
IPR011009 (Kinase-like_dom.)
IPR013783 (Ig-like_fold.)
IPR016246 (Tyr_kinase_insulin-like_rcpt.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR032675 (L_dom-like.)
Pfam PF00757 (Furin-like)
PF01030 (Recep_L_domain)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 1GAG 1I44 1IR3 1IRK 1P14 1RQQ 2AUH 2B4S 2HR7 2Z8C 3BU3 3BU5 3BU6 3EKK 3EKN 3ETA 3W11 3W12 3W13 3W14 4IBM 4OGA 4XLV 4XSS More...
CREDO 1GAG 1I44 1IR3 1IRK 1P14 1RQQ 2AUH 2B4S 2HR7 2Z8C 3BU3 3BU5 3BU6 3EKK 3EKN 3ETA 3W11 3W12 3W13 3W14 4IBM 4OGA 4XLV 4XSS More...
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