AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: zafirlukast
Target: Sodium/bile acid cotransporter (Transporter)
Gene: SLC10A1
UniProt: Q14973 (NTCP_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.19
Assay: Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method
Drug: zafirlukast
Target: Prostaglandin E synthase (Enzyme)
Gene: PTGES
UniProt: O14684 (PTGES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.74
Assay: Inhibition of microsomal PGES1 in ILbeta/TNFalpha-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by LC-MS/MS analysis
Drug: zalcitabine
Target: Deoxycytidine kinase (Kinase)
Gene: DCK
UniProt: P27707 (DCK_HUMAN)
Organism: Homo sapiens
Drug: zalcitabine
Target: Reverse transcriptase/RNaseH (Enzyme)
Gene: pol
UniProt: Q72547 (Q72547_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: Ki = 7.29
Action type: INHIBITOR
Assay: Inhibitory constant against HIV-1 reverse transcriptase
Drug: zaleplon
Target: GABA-A receptor alpha-2/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA2
UniProt: P18507|P28472|P47869 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.789
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: zaleplon
Target: GABA-A receptor alpha-1/beta-2/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB2
UniProt: P14867|P18507|P47870 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.53
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: P16207 (NRAM_INBVI)
Organism: Influenza B virus (strain B/Victoria/3/1985)
Activity: IC50 = 8.4
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: P03468 (NRAM_I34A1)
Organism: Influenza A virus (strain A/Puerto Rico/8/1934 H1N1)
Activity: IC50 = 9.3
Action type: INHIBITOR
Assay: Inhibitory activity was determined against Neuraminidase A from influenza virus A/Tokyo/3/67
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: P03474 (NRAM_INBLE)
Organism: Influenza B virus (strain B/Lee/1940)
Activity: Ki = 10
Action type: INHIBITOR
Assay: Inhibition of influenza B/Memphis/3/89 neuraminidase
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: B4URF0 (B4URF0_9INFA)
Organism: Influenza A virus (A/WSN/1933(H1N1))
Activity: IC50 = 8.62
Assay: Inhibition of influenza A virus A/WSN/1933 H1N1 neuraminidase using NA-STAR substrate after 15 mins incubation at room temperature by fluorescent assay
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: Q75VQ4 (NRAM_I68A0)
Organism: Influenza A virus (strain A/Aichi/2/1968 H3N2)
Activity: IC50 = 8.58
Assay: Inhibition of human influenza A virus A/Aichi/2/1968(H3N2) neuraminidase by fluorometric method using 4MU-NeuAc substrate
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: Q6Q793 (Q6Q793_9INFA)
Organism: Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1))
Activity: Ki = 9.3
Assay: Inhibition of Influenza A virus (A/Thailand/1(KAN-1)/2004(H5N1)) neuraminidase by by Michaelis-Menten equation analysis
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: A5Z252 (A5Z252_9INFA)
Organism: Influenza A virus (A/Turkey/651242/2006(H5N1))
Activity: Ki = 9
Assay: Inhibition of Influenza A virus (A/Turkey/651242/2006(H5N1)) neuraminidase by Michaelis-Menten equation analysis
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: Q2LFS1 (Q2LFS1_9INFA)
Organism: Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1))
Activity: Ki = 9.4
Assay: Inhibition of Influenza A virus (A/chicken/Yogjakarta/BBVet-IX/2004(H5N1)) neuraminidase by Michaelis-Menten equation analysis
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: C4LRQ6 (C4LRQ6_9INFA)
Organism: Influenza A virus (A/duck/Laos/25/2006(H5N1))
Activity: Ki = 9.3
Assay: Inhibition of Influenza A virus (A/duck/Laos/25/2006(H5N1)) neuraminidase by Michaelis-Menten equation analysis
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: Q20MD3 (Q20MD3_9INFA)
Organism: Influenza A virus (A/udorn/1972(H3N2))
Activity: IC50 = 7.64
Assay: Inhibition of Influenza A virus A/Udorn/1972(H3N2) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: P03470 (NRAM_I33A0)
Organism: Influenza A virus (strain A/Wilson-Smith/1933 H1N1)
Activity: IC50 = 8.54
Assay: Inhibition of wild type Influenza A virus A/WSN/1933(H1N1) neuraminidase in virus-infected allantoic fluid using 2'-(4-methylumbelliferyl)-alpha-D-N-acetylneuraminic acid as substrate incubated for 10 mins prior to substrate addition by fluorescence assay
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: Q194T1 (Q194T1_9INFA)
Organism: Influenza A virus (A/RI/5+/1957(H2N2))
Activity: IC50 = 5.85
Assay: Inhibition of Influenza A virus (A/RI/5+/1957(H2N2)) recombinant neuraminidase using MUNANA as substrate after 30 mins
Drug: zanamivir
Target: Sialidase 3 (Enzyme)
Gene: NEU3
UniProt: Q9UQ49 (NEUR3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.17
Assay: Inhibition of human NEU3 expressed in HEK293 cells by fluorometric high-performance liquid chromatography using ganglioside GM3 substrate
Drug: zanamivir
Target: Sialidase 2 (Enzyme)
Gene: NEU2
UniProt: Q9Y3R4 (NEUR2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.77
Assay: Inhibition of human neuraminidase 2
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: Q07599 (NRAM_I63A3)
Organism: Influenza A virus (strain A/Duck/Ukraine/1/1963 H3N8)
Activity: IC50 = 8.13
Assay: Inhibition of Influenza A virus A/goose/Jiangsu/1306/2014(H5N8) neuraminidase N8 using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: Q3S340 (Q3S340_9INFB)
Organism: Influenza B virus (B/Perth/211/2001)
Activity: IC50 = 8.05
Assay: Inhibition of Influenza B virus (B/Perth/211/2001) neuraminidase activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay
Drug: zanamivir
Target: Sialidase-4 (Enzyme)
Gene: NEU4
UniProt: Q8WWR8 (NEUR4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.58
Assay: Inhibition of human N-terminal MBP-fused NEU4 expressed in Escherichia coli using 4MU-NANA as substrate preincubated for 15 mins followed by substrate addition measured every minute for 30 mins by fluorescence based assay
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: D5F1R0 (D5F1R0_9INFA)
Organism: Influenza A virus
Activity: IC50 = 8.47
Assay: Inhibition of Influenza A virus (A/Fukui/45/04(H3N2)) neuraminidase E119V mutant activity using 4-MUNANA as substrate preincubated for 60 mins followed by substrate addition measured every min for 60 mins by fluorescence assay
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: P03471 (NRAM_I71A1)
Organism: Influenza A virus
Activity: IC50 = 8.76
Assay: Inhibition of Influenza A virus A/Memphis/1/71(H3N2) sialidase preincubated for 15 mins followed by MUNA substrate addition measured after 15 mins by fluorescence assay
Drug: zanamivir
Target: Neuraminidase (Enzyme)
UniProt: Q6XV28 (NRAM_I77AG)
Organism: Influenza A virus
Activity: IC50 = 7.64
Assay: Inhibition of Influenza A virus A/duck/Guangdong/674/2014(H5N6) neuraminidase N6 using fluorogenic MUNANA as substrate preincubated for 10 mins followed by substrate addition measured after 40 to 60 mins by fluorescence-based assay
Drug: zidovudine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4
Drug: zidovudine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.51
Drug: zidovudine
Target: Thymidine kinase, cytosolic (Kinase)
Gene: TK1
UniProt: P04183 (KITH_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.54
Assay: Inhibitory affect against rabbit thymus thymidine kinase and represented as molt/4F kinase.
Drug: zidovudine
Target: Thymidylate kinase (Kinase)
Gene: DTYMK
UniProt: P23919 (KTHY_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.55
Drug: zidovudine
Target: Pol polyprotein (Enzyme)
Gene: pol
UniProt: Q72874 (Q72874_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 8.22
Assay: Inhibitory effect on HIV-1 RT activity using template primer,poly (rA)-oligo (dT)
Drug: zidovudine
Target: Reverse transcriptase/RNaseH (Enzyme)
Gene: pol
UniProt: Q72547 (Q72547_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 8.52
Action type: INHIBITOR
Assay: Inhibitory concentration against human immunodeficiency virus type 1 (HIV-1 strain IIIB RT) reverse transcriptase was determined by triplicate assay at low (~0.1 pfu/cell) multiplicity of injection (moi)
Drug: zidovudine
Target: Gag-Pro-Pol polyprotein (Polyprotein)
Gene: gag-pro-pol
UniProt: P03362 (POL_HTL1A)
Organism: Human T-cell leukemia virus 1 (strain Japan ATK-1 subtype A)
Activity: EC50 = 8.31
Drug: zidovudine
Target: Reverse transcriptase/RNaseH (Enzyme)
Gene: pol
UniProt: Q72549 (Q72549_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 6.11
Drug: zidovudine
Target: Reverse transcriptase (Enzyme)
Gene: reverse transcriptas
UniProt: Q9WKE8 (Q9WKE8_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 4.74
Drug: zidovudine
Target: Thymidylate kinase (Kinase)
Gene: tmk
UniProt: P9WKE1 (KTHY_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Activity: Ki = 4.55
Assay: Inhibitory activity against thymidine monophosphate kinase (TMPK) in Mycobacterium tuberculosis
Drug: zidovudine
Target: Thymidine kinase (Kinase)
Gene: tdk
UniProt: Q9PPP5 (KITH_UREPA)
Organism: Ureaplasma parvum serovar 3 (strain ATCC 700970)
Activity: IC50 = 4.9
Assay: Inhibition of Ureaplasma parvum thymidine kinase by liquid scintillation counting
Drug: zidovudine
Target: Reverse transcriptase protein (Unclassified)
Gene: reverse transcriptase
UniProt: Q9WJQ2 (Q9WJQ2_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 5.44
Assay: Inhibition of HIV1 reverse transcriptase M184V mutant-mediated viral DNA synthesis in human HOS cells assessed as luciferase activity treated 3 hrs before infection measured after 48 hrs by luminescence assay
Drug: zileuton
Target: Arachidonate 5-lipoxygenase (Enzyme)
Gene: ALOX5
UniProt: P09917 (LOX5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.52
Action type: INHIBITOR
Assay: Inhibition of 5-LOX (unknown origin) using arachidonic acid as substrate after 5 mins by EIA
Drug: zileuton
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P16050 (LOX15_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.4
Assay: Inhibition of 15-LOX in human primary polymorphonuclear leukocytes
Drug: zileuton
Target: Cysteinyl leukotriene receptor 2 (GPCR)
Gene: CYSLTR2
UniProt: Q9NS75 (CLTR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.824
Drug: zileuton
Target: Leukotriene A-4 hydrolase (Enzyme)
Gene: LTA4H
UniProt: P09960 (LKHA4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.071
Drug: zileuton
Target: Leukotriene B4 receptor 1 (GPCR)
Gene: LTB4R
UniProt: Q15722 (LT4R1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.38
Assay: In vitro activities of Leukotriene B4 receptor (LTB4) in human neutrophils
Drug: zileuton
Target: Arachidonate 5-lipoxygenase-activating protein (Cytosolic other)
Gene: ALOX5AP
UniProt: P20292 (AL5AP_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.66
Assay: Inhibition of FLAP in human whole blood assessed as inhibition of calcium ionophore A23187-induced LTB4 production preincubated for 15 mins by ELISA
Drug: zileuton
Target: Bifunctional epoxide hydrolase 2 (Enzyme)
Gene: EPHX2
UniProt: P34913 (HYES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.23
Assay: Inhibition of human recombinant soluble epoxide hydrolase expressed in Escherichia coli using 3-phenyl-cyano(6-methoxy-2-naphthalenyl)methylester-2-oxiraneacetic acid as substrate after 30 mins by fluorescence-based assay
Drug: zileuton
Target: Arachidonate 5-lipoxygenase (Enzyme)
Gene: Alox5
UniProt: P12527 (LOX5_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.85
Assay: Inhibition of 5-Lipoxygenase of rat basophilic leukemia cells
Drug: zileuton
Target: Arachidonate 5-lipoxygenase (Enzyme)
Gene: Alox5
UniProt: P48999 (LOX5_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.72
Drug: zileuton
Target: Prostaglandin E synthase (Enzyme)
Gene: PTGES
UniProt: O14684 (PTGES_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.22
Assay: Inhibition of mPGES-1 isolated from microsomes of interleukin-1 beta-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis
Drug: zimeldine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.727
Drug: zimeldine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.818
Drug: zimeldine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.027
Drug: ziprasidone
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.59
Drug: ziprasidone
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: ziprasidone
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.02
Assay: Binding affinity against dopamine receptor D1
Drug: ziprasidone
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.32
Action type: ANTAGONIST
Drug: ziprasidone
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Drug: ziprasidone
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.92
Drug: ziprasidone
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7
Drug: ziprasidone
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.357
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.47
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.4
Action type: ANTAGONIST
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.565
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.89
Action type: ANTAGONIST
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.22
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Drug: ziprasidone
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Drug: ziprasidone
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.319
Drug: ziprasidone
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.14
Action type: ANTAGONIST
Drug: ziprasidone
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.818
Drug: ziprasidone
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.33
Drug: ziprasidone
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.456
Drug: ziprasidone
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.55
Drug: ziprasidone
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.523
Drug: ziprasidone
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5
Drug: ziprasidone
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.796
Drug: ziprasidone
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.796
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: AGONIST
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Drug: ziprasidone
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.114
Drug: ziprasidone
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Drug: ziprasidone
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.3
Action type: ANTAGONIST
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Drug: ziprasidone
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.046
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.536
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.44
Drug: ziprasidone
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.3
Assay: Displacement of [3H]prazosin from rat adrenergic alpha1A receptor expressed in fibroblast cells
Drug: ziprasidone
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 7.8
Drug: ziprasidone
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.32
Assay: Displacement of [3H]NPA from rat brain Dopamine receptor D2
Drug: ziprasidone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.38
Drug: ziprasidone
Target: Histamine H1 receptor (GPCR)
Gene: Hrh1
UniProt: P31390 (HRH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.82
Assay: Displacement of [3H]mepyramine from H1R in rat brain
Drug: ziprasidone
Target: Transporter (Transporter)
Gene: NET
UniProt: Q63380 (Q63380_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.32
Assay: Binding affinity to rat NET
Drug: ziprasidone
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.96
Assay: Displacement of [3H]prazosin from Alpha-1 adrenergic receptor in rat brain
Drug: ziprasidone
Target: Histone H1.0 (Nuclear other)
Gene: H1F0
UniProt: P07305 (H10_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.82
Assay: Binding Assay: Binding assay using 5-HT2A, Dopamine D2, SERT, αA1, 5-HT2C and H1 Receptors.
Drug: zofenopril
Target: Angiotensin-converting enzyme (Enzyme)
Gene: ACE
UniProt: P12822 (ACE_RABIT)
Organism: Oryctolagus cuniculus
Activity: Ki = 9.4
Drug: zofenopril
Target: Angiotensin-converting enzyme (Enzyme)
Gene: Ace
UniProt: P47820 (ACE_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.1
Drug: zofenopril
Target: Angiotensin-converting enzyme (Enzyme)
Gene: ACE
UniProt: P12821 (ACE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.4
Action type: INHIBITOR
Assay: Inhibitory activity against angiotensin I converting enzyme (ACE)
Drug: zoledronic acid
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.21
Assay: Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration method
Drug: zoledronic acid
Target: Carbonic anhydrase 9 (Enzyme)
Gene: CA9
UniProt: Q16790 (CAH9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.27
Assay: Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration method
Drug: zoledronic acid
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.5
Assay: Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration method
Drug: zoledronic acid
Target: Farnesyl pyrophosphate synthase (Enzyme)
Gene: FDPS
UniProt: P14324 (FPPS_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.15
Action type: INHIBITOR
Assay: Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins
Drug: zoledronic acid
Target: 72 kDa type IV collagenase (Enzyme)
Gene: MMP2
UniProt: P08253 (MMP2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.15
Assay: Inhibition of APMA-activated recombinant human MMP2 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate incubated for 30 mins prior to substrate addition measured after 2 to 4 hrs by fluorometric assay
Drug: zoledronic acid
Target: Carbonic anhydrase 14 (Enzyme)
Gene: CA14
UniProt: Q9ULX7 (CAH14_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.04
Assay: Inhibition of human recombinant carbonic anhydrase 14 preincubated for 15 mins by stopped flow CO2 hydration method
Drug: zoledronic acid
Target: Matrix metalloproteinase-14 (Enzyme)
Gene: MMP14
UniProt: P50281 (MMP14_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.9
Assay: Inhibition of MMP14 catalytic domain (unknown origin) using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate incubated for 30 mins prior to substrate addition measured after 2 to 4 hrs by fluorometric assay
Drug: zoledronic acid
Target: Matrix metalloproteinase-9 (Enzyme)
Gene: MMP9
UniProt: P14780 (MMP9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.28
Assay: Inhibition of MMP9 catalytic domain (unknown origin) using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate incubated for 30 mins prior to substrate addition measured after 2 to 4 hrs by fluorometric assay
Drug: zoledronic acid
Target: Neutrophil collagenase (Enzyme)
Gene: MMP8
UniProt: P22894 (MMP8_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.75
Assay: Inhibition of MMP8 catalytic domain (unknown origin) using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate incubated for 30 mins prior to substrate addition measured after 2 to 4 hrs by fluorometric assay
Drug: zoledronic acid
Target: Geranylgeranyl pyrophosphate synthase (Enzyme)
Gene: GGPS1
UniProt: O95749 (GGPPS_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.57
Assay: Binding affinity to human GGPPS
Drug: zoledronic acid
Target: Farnesyl diphosphate synthase (Enzyme)
Gene: ispA
UniProt: P22939 (ISPA_ECOLI)
Organism: Escherichia coli (strain K12)
Activity: IC50 = 5.96
Assay: Inhibition of Escherichia coli FPPS
Drug: zoledronic acid
Target: Farnesyl pyrophosphate synthase (Enzyme)
UniProt: Q0GKD7 (Q0GKD7_LEIDO)
Organism: Leishmania donovani
Activity: Ki = 7.96
Assay: Binding affinity towards Farnesyl diphosphate synthase from leishmania major