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Target Report Card

Target Name and Classification

Target ID CHEMBL4860
Target Type SINGLE PROTEIN
Preferred Name Apoptosis regulator Bcl-2
Synonyms Apoptosis regulator Bcl-2 | BCL2
Organism Homo sapiens
Species Group No
Protein Target Classification
  • ion channel > other ion channel > miscellaneous ion channel > bcl-2 family

Target Components

Component Description Relationship Accession
Apoptosis regulator Bcl-2 SINGLE PROTEIN P10415

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL3137309 VENETOCLAX Apoptosis regulator Bcl-2 inhibitor 4 FDA
CHEMBL2107358 OBATOCLAX MESYLATE Apoptosis regulator Bcl-2 inhibitor 3 PubMed PubMed PubMed
CHEMBL443684 NAVITOCLAX Apoptosis regulator Bcl-2 inhibitor 2 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000171791
Ensembl ENSG00000171791
GO Cellular Component GO:0005622 (intracellular)
GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005741 (mitochondrial outer membrane)
GO:0005783 (endoplasmic reticulum)
GO:0005789 (endoplasmic reticulum membrane)
GO:0005829 (cytosol)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0031965 (nuclear membrane)
GO:0031966 (mitochondrial membrane)
GO:0043209 (myelin sheath)
GO:0046930 (pore complex)
GO Molecular Function GO:0002020 (protease binding)
GO:0005515 (protein binding)
GO:0008134 (transcription factor binding)
GO:0015267 (channel activity)
GO:0016248 (channel inhibitor activity)
GO:0019903 (protein phosphatase binding)
GO:0031625 (ubiquitin protein ligase binding)
GO:0042802 (identical protein binding)
GO:0042803 (protein homodimerization activity)
GO:0043565 (sequence-specific DNA binding)
GO:0046982 (protein heterodimerization activity)
GO:0051434 (BH3 domain binding)
GO:0051721 (protein phosphatase 2A binding)
GO Biological Process GO:0000209 (protein polyubiquitination)
GO:0000902 (cell morphogenesis)
GO:0001503 (ossification)
GO:0001541 (ovarian follicle development)
GO:0001656 (metanephros development)
GO:0001657 (ureteric bud development)
GO:0001658 (branching involved in ureteric bud morphogenesis)
GO:0001662 (behavioral fear response)
GO:0001776 (leukocyte homeostasis)
GO:0001782 (B cell homeostasis)
GO:0001822 (kidney development)
GO:0001836 (release of cytochrome c from mitochondria)
GO:0001952 (regulation of cell-matrix adhesion)
GO:0002260 (lymphocyte homeostasis)
GO:0002320 (lymphoid progenitor cell differentiation)
GO:0002326 (B cell lineage commitment)
GO:0002360 (T cell lineage commitment)
GO:0002520 (immune system development)
GO:0002931 (response to ischemia)
GO:0003014 (renal system process)
GO:0006470 (protein dephosphorylation)
GO:0006582 (melanin metabolic process)
GO:0006808 (regulation of nitrogen utilization)
GO:0006874 (cellular calcium ion homeostasis)
GO:0006915 (apoptotic process)
GO:0006959 (humoral immune response)
GO:0006974 (cellular response to DNA damage stimulus)
GO:0006979 (response to oxidative stress)
GO:0007015 (actin filament organization)
GO:0007409 (axonogenesis)
GO:0007565 (female pregnancy)
GO:0007569 (cell aging)
GO:0008283 (cell proliferation)
GO:0008284 (positive regulation of cell proliferation)
GO:0008285 (negative regulation of cell proliferation)
GO:0008584 (male gonad development)
GO:0008625 (extrinsic apoptotic signaling pathway via death domain receptors)
GO:0008630 (intrinsic apoptotic signaling pathway in response to DNA damage)
GO:0008631 (intrinsic apoptotic signaling pathway in response to oxidative stress)
GO:0008637 (apoptotic mitochondrial changes)
GO:0009314 (response to radiation)
GO:0009636 (response to toxic substance)
GO:0009791 (post-embryonic development)
GO:0009887 (organ morphogenesis)
GO:0010039 (response to iron ion)
GO:0010224 (response to UV-B)
GO:0010332 (response to gamma radiation)
GO:0010468 (regulation of gene expression)
GO:0010506 (regulation of autophagy)
GO:0010507 (negative regulation of autophagy)
GO:0010523 (negative regulation of calcium ion transport into cytosol)
GO:0010559 (regulation of glycoprotein biosynthetic process)
GO:0014031 (mesenchymal cell development)
GO:0014042 (positive regulation of neuron maturation)
GO:0014911 (positive regulation of smooth muscle cell migration)
GO:0016049 (cell growth)
GO:0016337 (single organismal cell-cell adhesion)
GO:0018105 (peptidyl-serine phosphorylation)
GO:0018107 (peptidyl-threonine phosphorylation)
GO:0021747 (cochlear nucleus development)
GO:0022612 (gland morphogenesis)
GO:0022898 (regulation of transmembrane transporter activity)
GO:0030097 (hemopoiesis)
GO:0030183 (B cell differentiation)
GO:0030217 (T cell differentiation)
GO:0030279 (negative regulation of ossification)
GO:0030307 (positive regulation of cell growth)
GO:0030308 (negative regulation of cell growth)
GO:0030318 (melanocyte differentiation)
GO:0030336 (negative regulation of cell migration)
GO:0030890 (positive regulation of B cell proliferation)
GO:0031069 (hair follicle morphogenesis)
GO:0031103 (axon regeneration)
GO:0031647 (regulation of protein stability)
GO:0032469 (endoplasmic reticulum calcium ion homeostasis)
GO:0032835 (glomerulus development)
GO:0032848 (negative regulation of cellular pH reduction)
GO:0032880 (regulation of protein localization)
GO:0033033 (negative regulation of myeloid cell apoptotic process)
GO:0033077 (T cell differentiation in thymus)
GO:0033138 (positive regulation of peptidyl-serine phosphorylation)
GO:0033689 (negative regulation of osteoblast proliferation)
GO:0034097 (response to cytokine)
GO:0035094 (response to nicotine)
GO:0035265 (organ growth)
GO:0040007 (growth)
GO:0040018 (positive regulation of multicellular organism growth)
GO:0042100 (B cell proliferation)
GO:0042149 (cellular response to glucose starvation)
GO:0042493 (response to drug)
GO:0042542 (response to hydrogen peroxide)
GO:0042981 (regulation of apoptotic process)
GO:0043029 (T cell homeostasis)
GO:0043066 (negative regulation of apoptotic process)
GO:0043067 (regulation of programmed cell death)
GO:0043085 (positive regulation of catalytic activity)
GO:0043375 (CD8-positive, alpha-beta T cell lineage commitment)
GO:0043473 (pigmentation)
GO:0043496 (regulation of protein homodimerization activity)
GO:0043497 (regulation of protein heterodimerization activity)
GO:0043524 (negative regulation of neuron apoptotic process)
GO:0043583 (ear development)
GO:0045069 (regulation of viral genome replication)
GO:0045636 (positive regulation of melanocyte differentiation)
GO:0045930 (negative regulation of mitotic cell cycle)
GO:0046671 (negative regulation of retinal cell programmed cell death)
GO:0046902 (regulation of mitochondrial membrane permeability)
GO:0048041 (focal adhesion assembly)
GO:0048066 (developmental pigmentation)
GO:0048070 (regulation of developmental pigmentation)
GO:0048087 (positive regulation of developmental pigmentation)
GO:0048536 (spleen development)
GO:0048538 (thymus development)
GO:0048545 (response to steroid hormone)
GO:0048546 (digestive tract morphogenesis)
GO:0048589 (developmental growth)
GO:0048599 (oocyte development)
GO:0048743 (positive regulation of skeletal muscle fiber development)
GO:0048753 (pigment granule organization)
GO:0048873 (homeostasis of number of cells within a tissue)
GO:0050790 (regulation of catalytic activity)
GO:0050853 (B cell receptor signaling pathway)
GO:0051384 (response to glucocorticoid)
GO:0051402 (neuron apoptotic process)
GO:0051607 (defense response to virus)
GO:0051726 (regulation of cell cycle)
GO:0051881 (regulation of mitochondrial membrane potential)
GO:0051902 (negative regulation of mitochondrial depolarization)
GO:0051924 (regulation of calcium ion transport)
GO:0055085 (transmembrane transport)
GO:0070059 (intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stress)
GO:0071310 (cellular response to organic substance)
GO:0071456 (cellular response to hypoxia)
GO:0072593 (reactive oxygen species metabolic process)
GO:0097192 (extrinsic apoptotic signaling pathway in absence of ligand)
GO:1900740 (positive regulation of protein insertion into mitochondrial membrane involved in apoptotic signaling pathway)
GO:2000134 (negative regulation of G1/S transition of mitotic cell cycle)
GO:2000378 (negative regulation of reactive oxygen species metabolic process)
GO:2000811 (negative regulation of anoikis)
GO:2001234 (negative regulation of apoptotic signaling pathway)
GO:2001240 (negative regulation of extrinsic apoptotic signaling pathway in absence of ligand)
GO:2001243 (negative regulation of intrinsic apoptotic signaling pathway)
GO:2001244 (positive regulation of intrinsic apoptotic signaling pathway)
Wikipedia Bcl-2

Target Cross References - Protein

canSAR P10415
Human Protein Atlas ENSG00000171791
IntAct P10415
Guide to Pharmacology 2844
Open Targets ENSG00000171791
PharmGKB PA25302
Reactome R-HSA-111447 (Activation of BAD and translocation to mitochondria.)
R-HSA-111453 (BH3-only proteins associate with and inactivate anti-apoptotic BCL-2 members.)
R-HSA-6785807 (Interleukin-4 and 13 signaling.)
R-HSA-844455 (The NLRP1 inflammasome.)
TIMBAL Bcl-XL%20and%20Bcl-2
UniProt C9JHD5 P10415 P10416 Q13842 Q16197

Target Cross References - Domain

InterPro IPR002475 (Bcl2-like.)
IPR003093 (Bcl2_BH4.)
IPR004725 (Bcl2/BclX.)
IPR013278 (Apop_reg_Bcl2.)
IPR020717 (Bcl2_BH1_motif_CS.)
IPR020726 (Bcl2_BH2_motif_CS.)
IPR020728 (Bcl2_BH3_motif_CS.)
IPR020731 (Bcl2_BH4_motif_CS.)
IPR026298 (Blc2_fam.)
Pfam PF00452 (Bcl-2)
PF02180 (BH4)

Target Cross References - Structure

PDBe 2W3L 2XA0 4AQ3 4IEH 4LVT 4LXD 4MAN 5AGW 5AGX 5FCG 5JSN
CREDO 2W3L 2XA0 4AQ3 4IEH 4LVT 4LXD 4MAN 5AGW 5AGX 5FCG 5JSN
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