Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T85605 Target Info
Target Name 5-HT receptor (5HTR)
Synonyms
5-Hydroxytryptamine receptor
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Target Type Successful Target
Gene Name NO-GeName
Biochemical Class GPCR rhodopsin
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
Co-Target Name Muscarinic acetylcholine receptor M1 (CHRM1) Successful Target
UniProt ID ACM1_HUMAN
Gene Name CHRM1
Synonyms
M1 receptor
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Representative Drug(s) Pizotyline Drug Info Ki = 2 nM [1]
Co-Target Name Dopamine D2 receptor (D2R) Successful Target
UniProt ID DRD2_HUMAN
Gene Name DRD2
Synonyms
Dopamine receptor 2; D(2) dopamine receptor
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Representative Drug(s) Pizotyline Drug Info Ki = 2.4 nM Click to Show More [1]
2 Paliperidone Drug Info IC50 = 8.28 nM [3]
3 Tandospirone Drug Info Ki = 460 nM [2]
Co-Target Name Dopamine D4 receptor (D4R) Successful Target
UniProt ID DRD4_HUMAN
Gene Name DRD4
Synonyms
DRD4; D(2C)D(4) dopamine receptor dopamine receptor
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Representative Drug(s) Tandospirone Drug Info Ki = 7.2 nM [2]
Co-Target Name Cyclin-dependent kinase 4 (CDK4) Successful Target
UniProt ID CDK4_HUMAN
Gene Name CDK4
Synonyms
PSK-J3; Cell division protein kinase 4
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Representative Drug(s) Palbociclib Drug Info IC50 = 9 nM [4]
Co-Target Name Cyclin-dependent kinase 6 (CDK6) Successful Target
UniProt ID CDK6_HUMAN
Gene Name CDK6
Synonyms
Serine/threonine-protein kinase PLSTIRE; Serine/threonine protein kinase PLSTIRE; Cell division protein kinase 6; CDKN6
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Representative Drug(s) Palbociclib Drug Info IC50 = 15 nM [4]
Co-Target Name Janus kinase 3 (JAK-3) Successful Target
UniProt ID JAK3_HUMAN
Gene Name JAK3
Synonyms
Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK
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Representative Drug(s) Palbociclib Drug Info IC50 = 63.1 nM [5]
Co-Target Name Voltage-gated potassium channel Kv11.1 (KCNH2) Successful Target
UniProt ID KCNH2_HUMAN
Gene Name KCNH2
Synonyms
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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Representative Drug(s) Paliperidone Drug Info IC50 = 1000 nM [6]
Co-Target Name Positive transcription elongation factor b (P-TEFb) Clinical trial Target
UniProt ID CDK9_HUMAN-CCNT1_HUMAN
Gene Name CDK9-CCNT1
Synonyms
P-TEFb
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Representative Drug(s) Palbociclib Drug Info Ki = 364 nM [7]
Co-Target Name Cyclin-dependent kinase 9 (CDK9) Clinical trial Target
UniProt ID CDK9_HUMAN
Gene Name CDK9
Synonyms
Tat-associated kinase complex catalytic subunit; TAK; Similar to cyclin-dependent kinase 9; Serine/threonine-protein kinase PITALRE; Cyclin-dependent protein kinase Cdk9; Cell division protein kinase 9; Cell division cycle 2-like protein kinase 4; CDC2L4; CDC2-related kinase; C-2K
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Representative Drug(s) Palbociclib Drug Info IC50 = 794.33 nM [5]
Co-Target Name HUAMN alpha-1 adrenergic receptor (ADRA1) Literature-reported Target
UniProt ID ADA1A_HUMAN; ADA1B_HUMAN; ADA1D_HUMAN
Gene Name ADRA1A; ADRA1B; ADRA1D
Synonyms
Alpha-1 adrenoreceptor
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Representative Drug(s) Pizotyline Drug Info Ki = 75 nM [1]
Co-Target Name Cyclin dependent kinase 4-G1/S specific cyclin D1 complex (CDK4-CCND1) Co-Target
UniProt ID CDK4_HUMAN-CCND1_HUMAN
Gene Name CDK4-CCND1
Representative Drug(s) Palbociclib Drug Info IC50 = 2 nM [8]
Co-Target Name Cyclin dependent kinase 6-G1/S specific cyclin D1 complex (CDK6-CCND1) Co-Target
UniProt ID CDK6_HUMAN-CCND1_HUMAN
Gene Name CDK6-CCND1
Representative Drug(s) Palbociclib Drug Info IC50 = 3.76 nM [9]
Co-Target Name Cyclin dependent kinase 6-G1/S specific cyclin D2 complex (CDK6-CCND2) Co-Target
UniProt ID CDK6_HUMAN-CCND2_HUMAN
Gene Name CDK6-CCND2
Representative Drug(s) Palbociclib Drug Info IC50 = 9 nM [10]
Co-Target Name Cyclin dependent kinase 4-G1/S specific cyclin D complex (CDK4-CCND) Co-Target
UniProt ID CDK4_HUMAN-CCND1_HUMAN/CCND2_HUMAN/CCND3_HUMAN
Gene Name CDK4-CCND1-CCND2/CCND3
Representative Drug(s) Palbociclib Drug Info IC50 = 11 nM [11]
Co-Target Name Cyclin dependent kinase 6-G1/S specific cyclin D3 complex (CDK6-CCND2) Co-Target
UniProt ID CDK6_HUMAN-CCND3_HUMAN
Gene Name CDK6-CCND3
Representative Drug(s) Palbociclib Drug Info IC50 = 19 nM [12]
Co-Target Name Cyclin dependent kinase 2-Cyclin A2 complex (CDK2-CCNA2) Co-Target
UniProt ID CDK2_HUMAN-CCNA2_HUMAN
Gene Name CDK2-CCNA2
Representative Drug(s) Palbociclib Drug Info IC50 = 230 nM [9]
References  Top
REF 1 Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists. Bioorg Med Chem. 2013 Dec 15;21(24):7841-52.
REF 2 Conformational analysis of tandospirone in aqueous solution: lead evolution of potent dopamine D4 receptor ligands. Bioorg Med Chem Lett. 2001 May 7;11(9):1141-4.
REF 3 Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics. Bioorg Med Chem. 2017 Sep 1;25(17):4904-16.
REF 4 Third-generation CDK inhibitors: A review on the synthesis and binding modes of Palbociclib, Ribociclib and Abemaciclib. Eur J Med Chem. 2019 Jun 15;172:143-153.
REF 5 Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002.
REF 6 Prediction of Thorough QT study results using action potential simulations based on ion channel screens. J Pharmacol Toxicol Methods. Nov-Dec 2014;70(3):246-54.
REF 7 Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. J Med Chem. 2017 Mar 9;60(5):1892-915.
REF 8 Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. J Med Chem. 2014 Apr 24;57(8):3430-49.
REF 9 Discovery of 8-cyclopentyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-7-oxo-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carbonitrile (7x) as a potent inhibitor of cyclin-dependent kinase 4 (CDK4) and AMPK-related kinase 5 (ARK5). J Med Chem. 2014 Feb 13;57(3):578-99.
REF 10 Cyclin dependent kinase (CDK) inhibitors as anticancer drugs. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3420-35.
REF 11 Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. J Med Chem. 2005 Apr 7;48(7):2388-406.
REF 12 A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. Eur J Med Chem. 2018 Jan 20;144:1-28.

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