Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T24983 | Target Info | |||
Target Name | Dopamine D4 receptor (D4R) | ||||
Synonyms |
DRD4; D(2C)D(4) dopamine receptor dopamine receptor
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Target Type | Successful Target | ||||
Gene Name | DRD4 | ||||
Biochemical Class | GPCR rhodopsin | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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) | Drug Info | Ki = 0.98 nM | [1] | |||
Co-Target Name | Histamine H1 receptor (H1R) | Successful Target | ||||
UniProt ID | HRH1_HUMAN | |||||
Gene Name | HRH1 | |||||
Synonyms |
HH1R; H1R
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Representative Drug(s) | Drug Info | Ki = 1 nM | [2] | |||
Co-Target Name | 5-HT 2A receptor (HTR2A) | Successful Target | ||||
UniProt ID | 5HT2A_HUMAN | |||||
Gene Name | HTR2A | |||||
Synonyms |
Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2
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Representative Drug(s) | Drug Info | Ki = 2.692 nM | Click to Show More | [3] | ||
2 | L-745,870 | Drug Info | Ki = 200 nM | [13] | ||
Co-Target Name | 5-HT 2C receptor (HTR2C) | Successful Target | ||||
UniProt ID | 5HT2C_HUMAN | |||||
Gene Name | HTR2C | |||||
Synonyms |
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
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Representative Drug(s) | Drug Info | Ki = 2.884 nM | [4] | |||
Co-Target Name | Adrenergic receptor alpha-2C (ADRA2C) | Successful Target | ||||
UniProt ID | ADA2C_HUMAN | |||||
Gene Name | ADRA2C | |||||
Synonyms |
Subtype C4; Alpha-2CAR; Alpha-2C adrenoreceptor; Alpha-2C adrenoceptor; Alpha-2C adrenergic receptor; Alpha-2 adrenergic receptor subtype C4; ADRA2RL2; ADRA2L2
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Representative Drug(s) | Drug Info | Ki = 2.9 nM | Click to Show More | [5] | ||
2 | L-745,870 | Drug Info | Ki = 230 nM | [13] | ||
Co-Target Name | 5-HT 2B receptor (HTR2B) | Successful Target | ||||
UniProt ID | 5HT2B_HUMAN | |||||
Gene Name | HTR2B | |||||
Synonyms |
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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Representative Drug(s) | Drug Info | Ki = 3.162 nM | [6] | |||
Co-Target Name | 5-HT 2 receptor (5HT2R) | Successful Target | ||||
UniProt ID | 5HT2A_HUMAN; 5HT2B_HUMAN; 5HT2C_HUMAN | |||||
Gene Name | NO-GeName | |||||
Synonyms |
Serotonin receptor 2; 5-hydroxytryptamine receptor 2; 5-HT2 receptor
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Representative Drug(s) | Drug Info | Ki = 5.012 nM | Click to Show More | [7] | ||
2 | L-745,870 | Drug Info | Ki = 200 nM | [1] | ||
Co-Target Name | 5-HT 1A receptor (HTR1A) | Successful Target | ||||
UniProt ID | 5HT1A_HUMAN | |||||
Gene Name | HTR1A | |||||
Synonyms |
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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Representative Drug(s) | Drug Info | Ki = 6.38 nM | Click to Show More | [4] | ||
2 | NGD 94-1 | Drug Info | Ki = 180 nM | [13] | ||
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) | Drug Info | Ki = 7.11 nM | Click to Show More | [4] | ||
2 | L-745,870 | Drug Info | Ki = 448 nM | [18] | ||
Co-Target Name | Dopamine D1 receptor (D1R) | Successful Target | ||||
UniProt ID | DRD1_HUMAN | |||||
Gene Name | DRD1 | |||||
Synonyms |
D(1A) dopamine receptor
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Representative Drug(s) | Drug Info | Ki = 7.5 nM | Click to Show More | [4] | ||
2 | Phenyltoloxamine | Drug Info | Ki = 343 nM | [16] | ||
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 | [8] | ||
Co-Target Name | Adrenergic receptor alpha-1B (ADRA1B) | Successful Target | ||||
UniProt ID | ADA1B_HUMAN | |||||
Gene Name | ADRA1B | |||||
Synonyms |
Alpha-1B adrenoreceptor; Alpha-1B adrenoceptor; Alpha-1B adrenergic receptor; Alpha 1B-adrenoreceptor; Alpha 1B-adrenoceptor
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Representative Drug(s) | Drug Info | Ki = 10 nM | [9] | |||
Co-Target Name | Adrenergic receptor alpha-1A (ADRA1A) | Successful Target | ||||
UniProt ID | ADA1A_HUMAN | |||||
Gene Name | ADRA1A | |||||
Synonyms |
Alpha-adrenergic receptor 1c; Alpha-1C adrenergic receptor; Alpha-1A adrenoreceptor; Alpha-1A adrenoceptor; Alpha-1A adrenergic receptor; Alpha adrenergic receptor 1c; Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; ADRA1C
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Representative Drug(s) | Drug Info | Ki = 10 nM | [9] | |||
Co-Target Name | Muscarinic acetylcholine receptor M4 (CHRM4) | Successful Target | ||||
UniProt ID | ACM4_HUMAN | |||||
Gene Name | CHRM4 | |||||
Synonyms |
M4 receptor; CHRM4
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Representative Drug(s) | Drug Info | Ki = 12.59 nM | [6] | |||
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 | [8] | ||
Co-Target Name | Adrenergic receptor alpha-2A (ADRA2A) | Successful Target | ||||
UniProt ID | ADA2A_HUMAN | |||||
Gene Name | ADRA2A | |||||
Synonyms |
Alpha-2AAR; Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2A adrenergic receptor; Alpha-2 adrenergic receptor subtype C10; ADRAR; ADRA2R
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Representative Drug(s) | Drug Info | Ki = 24 nM | Click to Show More | [5] | ||
2 | L-745,870 | Drug Info | Ki = 170 nM | [13] | ||
Co-Target Name | Muscarinic acetylcholine receptor (CHRM) | Successful Target | ||||
UniProt ID | ACM1_HUMAN; ACM2_HUMAN; ACM3_HUMAN; ACM4_HUMAN; ACM5_HUMAN | |||||
Gene Name | NO-GeName | |||||
Representative Drug(s) | Drug Info | Ki = 34 nM | [10] | |||
Co-Target Name | Adrenergic receptor Alpha-2 (ADRA2) | Successful Target | ||||
UniProt ID | ADA2A_HUMAN; ADA2B_HUMAN; ADA2C_HUMAN | |||||
Gene Name | NO-GeName | |||||
Synonyms |
Alpha-2 adrenergic receptor; Alpha(2)-adrenoceptor
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Representative Drug(s) | Drug Info | Ki = 51 nM | Click to Show More | [1] | ||
2 | Drug Info | Ki = 51 nM | [1] | |||
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 | [11] | ||
Co-Target Name | Dopamine D3 receptor (D3R) | Successful Target | ||||
UniProt ID | DRD3_HUMAN | |||||
Gene Name | DRD3 | |||||
Synonyms |
D(3) dopamine receptor
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Representative Drug(s) | Drug Info | Ki = 88 nM | Click to Show More | [12] | ||
2 | L-745,870 | Drug Info | Ki = 380.19 nM | [17] | ||
Co-Target Name | Adrenergic receptor alpha-2B (ADRA2B) | Successful Target | ||||
UniProt ID | ADA2B_HUMAN | |||||
Gene Name | ADRA2B | |||||
Synonyms |
Subtype C2; Alpha-2BAR; Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2B adrenergic receptor; Alpha-2 adrenergic receptor subtype C2; ADRA2RL1; ADRA2L1
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Representative Drug(s) | Drug Info | Ki = 100 nM | Click to Show More | [9] | ||
2 | L-745,870 | Drug Info | Ki = 160 nM | [13] | ||
Co-Target Name | Muscarinic acetylcholine receptor M2 (CHRM2) | Successful Target | ||||
UniProt ID | ACM2_HUMAN | |||||
Gene Name | CHRM2 | |||||
Synonyms |
M2 receptor; CHRM2
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Representative Drug(s) | Drug Info | Ki = 100 nM | [9] | |||
Co-Target Name | Muscarinic acetylcholine receptor M3 (CHRM3) | Successful Target | ||||
UniProt ID | ACM3_HUMAN | |||||
Gene Name | CHRM3 | |||||
Synonyms |
M3 receptor; CHRM3
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Representative Drug(s) | Drug Info | Ki = 100 nM | [9] | |||
Co-Target Name | Muscarinic acetylcholine receptor M5 (CHRM5) | Successful Target | ||||
UniProt ID | ACM5_HUMAN | |||||
Gene Name | CHRM5 | |||||
Synonyms |
CHRM5
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Representative Drug(s) | Drug Info | Ki = 100 nM | [9] | |||
Co-Target Name | Opioid receptor sigma 1 (OPRS1) | Successful Target | ||||
UniProt ID | SGMR1_HUMAN | |||||
Gene Name | SIGMAR1 | |||||
Synonyms |
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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Representative Drug(s) | L-745,870 | Drug Info | Ki = 130 nM | [1] | ||
Co-Target Name | 5-HT 3A receptor (HTR3A) | Successful Target | ||||
UniProt ID | 5HT3A_HUMAN | |||||
Gene Name | HTR3A | |||||
Synonyms |
Serotonin-gated ion channel receptor; Serotonin receptor 3A; HTR3; 5HT3R; 5-hydroxytryptamine receptor 3A; 5-HT3RA; 5-HT3A; 5-HT3-A; 5-HT 3A
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Representative Drug(s) | Drug Info | Ki = 186.21 nM | Click to Show More | [3] | ||
2 | NGD 94-1 | Drug Info | Ki = 750 nM | [13] | ||
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) | Drug Info | IC50 = 190.55 nM | [14] | |||
Co-Target Name | Dopamine D5 receptor (D5R) | Successful Target | ||||
UniProt ID | DRD5_HUMAN | |||||
Gene Name | DRD5 | |||||
Synonyms |
Dopamine receptor 5; DRD5; D1beta dopamine receptor; D(5)D(1B) dopamine receptor dopamine receptor; D(5) dopamine receptor
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Representative Drug(s) | Drug Info | Ki = 198 nM | Click to Show More | [15] | ||
2 | Phenyltoloxamine | Drug Info | Ki = 414 nM | [16] | ||
Co-Target Name | 5-HT 3 receptor (5HT3R) | Successful Target | ||||
UniProt ID | 5HT3A_HUMAN; 5HT3B_HUMAN; 5HT3C_HUMAN; 5HT3D_HUMAN; 5HT3E_HUMAN | |||||
Gene Name | NO-GeName | |||||
Synonyms |
5-hydroxytryptamine receptor type 3; 5-hydroxytryptamine receptor 3; 5-HT3R; 5-HT3 receptor; 5-HT-3
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Representative Drug(s) | Drug Info | Ki = 398.11 nM | [6] | |||
Co-Target Name | 5-HT 1B receptor (HTR1B) | Successful Target | ||||
UniProt ID | 5HT1B_HUMAN | |||||
Gene Name | HTR1B | |||||
Synonyms |
Serotonin receptor 1B; Serotonin 1D beta receptor; S12; HTR1DB; 5-hydroxytryptamine receptor 1B; 5-HT1B receptor; 5-HT1B; 5-HT-1D-beta; 5-HT-1B
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Representative Drug(s) | Drug Info | Ki = 1000 nM | [9] | |||
Co-Target Name | 5-HT 1D receptor (HTR1D) | Successful Target | ||||
UniProt ID | 5HT1D_HUMAN | |||||
Gene Name | HTR1D | |||||
Synonyms |
Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D
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Representative Drug(s) | Drug Info | Ki ~ 1000 nM | [9] | |||
Co-Target Name | 5-HT 1E receptor (HTR1E) | Successful Target | ||||
UniProt ID | 5HT1E_HUMAN | |||||
Gene Name | HTR1E | |||||
Synonyms |
Serotonin receptor 1E; S31; 5-hydroxytryptamine receptor 1E; 5-HT1E; 5-HT-1E; 5-HT 1E
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Representative Drug(s) | Drug Info | Ki = 1000 nM | [9] | |||
Co-Target Name | 5-HT 5A receptor (HTR5A) | Successful Target | ||||
UniProt ID | 5HT5A_HUMAN | |||||
Gene Name | HTR5A | |||||
Synonyms |
Serotonin receptor 5A; 5-hydroxytryptamine receptor 5A; 5-HT5A; 5-HT-5A; 5-HT-5; 5-HT 5A
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Representative Drug(s) | Drug Info | Ki = 1000 nM | [19] | |||
Co-Target Name | 5-HT 6 receptor (HTR6) | Clinical trial Target | ||||
UniProt ID | 5HT6R_HUMAN | |||||
Gene Name | HTR6 | |||||
Synonyms |
Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
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Representative Drug(s) | Drug Info | Ki = 4 nM | [20] | |||
Co-Target Name | 5-HT 7 receptor (HTR7) | Clinical trial Target | ||||
UniProt ID | 5HT7R_HUMAN | |||||
Gene Name | HTR7 | |||||
Synonyms |
Serotonin receptor 7; 5HT7; 5-hydroxytryptamine receptor 7; 5-HT7 receptor; 5-HT7; 5-HT-X; 5-HT-7
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Representative Drug(s) | Drug Info | Ki = 5.5 nM | Click to Show More | [21] | ||
2 | L-745,870 | Drug Info | Ki = 226.3 nM | [23] | ||
Co-Target Name | Histamine H4 receptor (H4R) | Clinical trial Target | ||||
UniProt ID | HRH4_HUMAN | |||||
Gene Name | HRH4 | |||||
Synonyms |
SP9144; Pfi-013; HH4R; H4 receptor; GPRv53; GPCR105; G protein-coupled receptor 105; AXOR35
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Representative Drug(s) | Drug Info | Ki = 177.83 nM | [22] | |||
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 | [24] | ||
Co-Target Name | Histamine H3 receptor (H3R) | Clinical trial Target | ||||
UniProt ID | HRH3_HUMAN | |||||
Gene Name | HRH3 | |||||
Synonyms |
Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
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Representative Drug(s) | Drug Info | Ki = 631 nM | [25] | |||
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 | [11] | ||
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) | Drug Info | Ki = 3.7 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 | [26] | ||
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 | [27] | ||
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 | [28] | ||
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 | [29] | ||
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 | [30] | ||
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 | [27] |
References | Top | ||||
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REF 13 | Return of D 4 Dopamine Receptor Antagonists in Drug Discovery. J Med Chem. 2017 Sep 14;60(17):7233-7243. | ||||
REF 14 | GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers. Eur J Med Chem. 2009 May;44(5):1926-32. | ||||
REF 15 | Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics. Bioorg Med Chem Lett. 2009 Jan 15;19(2):538-42. | ||||
REF 16 | Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 ... J Med Chem. 2004 Aug 12;47(17):4155-8. | ||||
REF 17 | 1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D. J Med Chem. 2018 Apr 26;61(8):3712-25. | ||||
REF 18 | Dopamine D4 ligands and models of receptor activation: 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole and related heteroarylmethylarylpiperazines exhibit a substituent effect responsible for additional efficacy tuning. J Med Chem. 2004 Apr 22;47(9):2348-55. | ||||
REF 19 | Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7). J Med Chem. 2003 Jul 3;46(14):2795-812. | ||||
REF 20 | Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects. Eur J Med Chem. 2018 Feb 10;145:790-804. | ||||
REF 21 | The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. Bioorg Med Chem Lett. 2014 Jan 15;24(2):576-9. | ||||
REF 22 | Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. J Med Chem. 2006 Jul 27;49(15):4512-6. | ||||
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