AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: cyclobenzaprine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.812
Drug: cyclobenzaprine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.244
Action type: ANTAGONIST
Drug: cyclobenzaprine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.839
Drug: cyclobenzaprine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.821
Drug: cyclobenzaprine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.829
Drug: cyclobenzaprine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.95
Drug: cyclobenzaprine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.222
Drug: cyclobenzaprine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki  8.222
Drug: cyclobenzaprine
Target: Aldehyde oxidase (Enzyme)
Gene: AOX1
UniProt: Q06278 (AOXA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.509
Drug: cyclobenzaprine
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.52
Drug: cyclofenil
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.58
Assay: Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay
Drug: cyclofenil
Target: Estrogen receptor (Nuclear other)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.58
Assay: Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay
Drug: cycloguanil
Target: Dihydrofolate reductase (Enzyme)
Gene: DHFR
UniProt: P00374 (DYR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.25
Assay: Binding affinity to human recombinant DHFR expressed in Escherichia coli BL21(DE3) by competitive binding assay
Drug: cycloguanil
Target: Dihydrofolate reductase (Enzyme)
UniProt: P16184 (DYR_PNECA)
Organism: Pneumocystis carinii
Activity: Ki = 7.63
Assay: Binding affinity was reported with purified recombinant Pneumocystis carinii Dihydrofolate reductase
Drug: cycloguanil
Target: Bifunctional dihydrofolate reductase-thymidylate synthase (Enzyme)
UniProt: P13922 (DRTS_PLAFK)
Organism: Plasmodium falciparum
Activity: Ki = 8.96
Action type: INHIBITOR
Assay: Inhibition constant against Plasmodium falciparum dihydrofolate reductase
Drug: cycloguanil
Target: Dihydrofolate reductase (Enzyme)
Gene: Dhfr
UniProt: Q920D2 (DYR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.96
Assay: Inhibitory activity against dihydrofolate reductase in rat liver.
Drug: cycloguanil
Target: Dihydrofolate reductase (Enzyme)
Gene: folA
UniProt: P00381 (DYR_LACCA)
Organism: Lactobacillus casei
Activity: Ki = 4.76
Assay: Inhibitory activity against Lactobacillus casei dihydrofolate reductase (DHFR)
Drug: cycloguanil
Target: Dihydrofolate reductase (Enzyme)
Gene: DHFR
UniProt: P00378 (DYR_CHICK)
Organism: Gallus gallus
Activity: Ki = 6.95
Assay: Inhibitory activity against isolated chicken liver dihydrofolate reductase (DHFR)
Drug: cycloguanil
Target: Dihydrofolate reductase (Enzyme)
Gene: dfrA17
UniProt: B0BL08 (B0BL08_ECOLX)
Organism: Escherichia coli
Activity: Ki = 5.99
Assay: Inhibition of Escherichia coli DHFR assessed as NADP formation by quadratic Morrison plot analysis
Drug: cyclopentolate
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL245; SINGLE PROTEIN
Drug: cyclophosphamide
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.68
Drug: cycloserine
Target: Glutamate receptor ionotropic, NMDA 2A (Ion channel)
Gene: GRIN2A
UniProt: Q12879 (NMDE1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.64
Drug: cycloserine
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.31
Drug: cycloserine
Target: Glutamate receptor ionotropic, NMDA 3A (Ion channel)
Gene: GRIN3A
UniProt: Q8TCU5 (NMD3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.64
Drug: cycloserine
Target: Glutamate receptor ionotropic, NMDA 2B (Ion channel)
Gene: GRIN2B
UniProt: Q13224 (NMDE2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.64
Drug: cycloserine
Target: Glutamate receptor ionotropic, NMDA 2C (Ion channel)
Gene: GRIN2C
UniProt: Q14957 (NMDE3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.34
Drug: cycloserine
Target: Glutamate receptor ionotropic, NMDA 2D (Ion channel)
Gene: GRIN2D
UniProt: O15399 (NMDE4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.64
Drug: cycloserine
Target: Alanine racemase (Enzyme)
Gene: alr
UniProt: P9WQA8 (ALR_MYCTO)
Organism: Mycobacterium tuberculosis (strain CDC 1551 / Oshkosh)
Drug: cycloserine
Target: Glutamate receptor ionotropic, NMDA 1 (Ion channel)
Gene: GRIN1
UniProt: Q05586 (NMDZ1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.26
Drug: cycloserine
Target: Glutamate receptor ionotropic, NMDA 3B (Ion channel)
Gene: GRIN3B
UniProt: O60391 (NMD3B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.64
Drug: cycloserine
Target: D-alanine--D-alanine ligase (Enzyme)
Gene: ddl
UniProt: P9WP31 (DDL_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2030; SINGLE PROTEIN
Drug: cycloserine
Target: Alanine racemase (Enzyme)
Gene: alr
UniProt: P9WQA9 (ALR_MYCTU)
Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2031; SINGLE PROTEIN
Drug: cycloserine
Target: Glutamate receptor ionotropic, NMDA 1 (Ion channel)
Gene: Grin1
UniProt: P35439 (NMDZ1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.13
Assay: In vitro inhibitory activity to inhibit [3H]glycine binding to NMDA receptor
Drug: cycloserine
Target: Glutamate receptor ionotropic, NMDA 2C (Ion channel)
Gene: Grin2c
UniProt: Q00961 (NMDE3_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 4.74
Assay: Compound was evaluated for in vitro inhibition of [3H]TCP at NMDA receptor.
Drug: cycloserine
Target: Glutamate NMDA receptor (Ion channel)
Gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3b|Grin3a
UniProt: P35439|Q00959|Q00960|Q00961|Q62645|Q8VHN2|Q9R1M7 (NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3B_RAT|NMD3A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.64
Assay: In vitro inhibition of [3H]glycine at NMDA receptor
Drug: ciclosporin
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.31
Drug: ciclosporin
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.301
Drug: ciclosporin
Target: Canalicular multispecific organic anion transporter 1 (Transporter)
Gene: ABCC2
UniProt: Q92887 (MRP2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.87
Assay: Inhibition of human MRP2 expressed in dog MDCK2 cells
Drug: ciclosporin
Target: Peptidyl-prolyl cis-trans isomerase FKBP1A (Enzyme)
Gene: FKBP1A
UniProt: P62942 (FKB1A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.796
Drug: ciclosporin
Target: Dihydroorotate dehydrogenase (quinone), mitochondrial (Enzyme)
Gene: DHODH
UniProt: Q02127 (PYRD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.699
Drug: ciclosporin
Target: Peptidyl-prolyl cis-trans isomerase A (Enzyme)
Gene: PPIA
UniProt: P62937 (PPIA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.046
Action type: MODULATOR
Drug: ciclosporin
Target: Multidrug resistance-associated protein 1 (Transporter)
Gene: ABCC1
UniProt: P33527 (MRP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.57
Assay: Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay
Drug: ciclosporin
Target: ATP-binding cassette sub-family G member 2 (Transporter)
Gene: ABCG2
UniProt: Q9UNQ0 (ABCG2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.2
Assay: Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay
Drug: ciclosporin
Target: fMet-Leu-Phe receptor (GPCR)
Gene: FPR1
UniProt: P21462 (FPR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.3
Action type: ANTAGONIST
Drug: ciclosporin
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Drug: ciclosporin
Target: Solute carrier organic anion transporter family member 1B1 (Transporter)
Gene: SLCO1B1
UniProt: Q9Y6L6 (SO1B1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.29
Action type: INHIBITOR
Drug: ciclosporin
Target: Peptidyl-prolyl cis-trans isomerase FKBP4 (Enzyme)
Gene: FKBP4
UniProt: Q02790 (FKBP4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.8
Assay: 50% inhibitory concentration of competitive binding against hCyp-18 PPIase activity using uncoupled assay
Drug: ciclosporin
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.86
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: ciclosporin
Target: Peptidyl-prolyl cis-trans isomerase B (Enzyme)
Gene: PPIB
UniProt: P23284 (PPIB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.01
Assay: Binding affinity to human Cyclophilin B
Drug: ciclosporin
Target: Serine/threonine-protein phosphatase 2B catalytic subunit alpha isoform (Enzyme)
Gene: PPP3CA
UniProt: Q08209 (PP2BA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.4
Assay: Binding affinity to protein phosphatase, calcineurin (CN) was determined
Drug: ciclosporin
Target: Reverse transcriptase/RNaseH (Enzyme)
Gene: pol
UniProt: Q72547 (Q72547_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 6.34
Assay: In vitro inhibitory activity against HIV-1 RT in CEM4 cell line
Drug: ciclosporin
Target: Peptidyl-prolyl cis-trans isomerase FKBP1B (Enzyme)
Gene: FKBP1B
UniProt: P68106 (FKB1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.22
Assay: The compound was tested for inhibition of Peptidyl-propyl isomerase (PPIase).
Drug: ciclosporin
Target: Peptidyl-prolyl cis-trans isomerase D (Enzyme)
Gene: PPID
UniProt: Q08752 (PPID_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.15
Assay: Inhibition of fluorescein labeled cyclosporin binding to Cyp40 by fluorescence polarization competition assay
Drug: ciclosporin
Target: Solute carrier organic anion transporter family member 1B3 (Transporter)
Gene: SLCO1B3
UniProt: Q9NPD5 (SO1B3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.1
Action type: INHIBITOR
Drug: ciclosporin
Target: Sodium/bile acid cotransporter (Transporter)
Gene: SLC10A1
UniProt: Q14973 (NTCP_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Drug: ciclosporin
Target: Bile salt export pump (Transporter)
Gene: Abcb11
UniProt: O70127 (ABCBB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.22
Drug: ciclosporin
Target: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Kinase)
Gene: Pik3cg
UniProt: Q9JHG7 (PK3CG_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.24
Assay: Inhibition of PI3K-gamma in mouse lymph node cells assessed as inhibition of ConA-stimulated T cell proliferation
Drug: cyclothiazide
Target: Solute carrier family 12 member 3 (Transporter)
Gene: SLC12A3
UniProt: P55017 (S12A3_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1876; SINGLE PROTEIN
Drug: cyclothiazide
Target: Glutamate receptor 1 (Ion channel)
Gene: GRIA1
UniProt: P42261 (GRIA1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.7
Assay: Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on 10 uM glutamate-induced current by voltage-clamp electrophysiological assay
Drug: cyclothiazide
Target: Glutamate receptor 2 (Ion channel)
Gene: GRIA2
UniProt: P42262 (GRIA2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.65
Assay: Activity at human recombinant GluA2 receptor flip isoform expressed in HEK293 cells assessed as effect on glutamate-induced calcium flux by Fluo-4/AM staining-based fluorescence assay
Drug: cyclothiazide
Target: Glutamate receptor 4 (Ion channel)
Gene: GRIA4
UniProt: P48058 (GRIA4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.41
Action type: ALLOSTERIC MODULATOR
Drug: cyclothiazide
Target: Glutamate receptor 3 (Ion channel)
Gene: GRIA3
UniProt: P42263 (GRIA3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.86
Action type: ALLOSTERIC MODULATOR
Drug: cyclothiazide
Target: Glutamate receptor ionotropic, AMPA (Ion channel)
Gene: Gria1|Gria2|Gria3|Gria4
UniProt: P19490|P19491|P19492|P19493 (GRIA1_RAT|GRIA2_RAT|GRIA3_RAT|GRIA4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.21
Assay: Inhibition of binding to AMPA receptor from rat cerebral cortex
Drug: cyclovalone
Target: Nuclear factor NF-kappa-B p105 subunit (Cytosolic other)
Gene: NFKB1
UniProt: P19838 (NFKB1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.38
Assay: Cellular Firefly Luciferase Assay (NFkB): The NF-kB activities of curcumin and analogs were determined by a cellular firefly luciferase assay. This assay utilized a commercially available cell line (Panomics 293T-luc cellular assay) developed for screening inhibitors of NF-kB. This cell line is stably transfected with a luciferase reporter controlled by an NF-kB dependent promoter. The cell is stimulated with tumor necrosis factor alpha (TNFalpha) which activates NF-kB. NF-kB then binds to one of six promoter regions on the cell's DNA leading to the production of a luciferase enzyme. Luciferin is added to the cell lysates and the luciferase enzyme catalyzes a cleavage of luciferin leading to the emission of light.
Drug: cyclovalone
Target: Integrase (Enzyme)
Gene: pol
UniProt: Q7ZJM1 (Q7ZJM1_9HIV1)
Organism: Human immunodeficiency virus 1
Activity: IC50 = 4
Assay: Inhibitory activity against HIV-1 Integrase (HIV-1-IN)
Drug: cyclovalone
Target: Transcription factor AP-1 (Transcription factor)
Gene: JUN
UniProt: P05412 (JUN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.14
Assay: Cellular Firefly Luciferase Assay (AP-1): Curcumin is a known inhibitor of the AP-1 activation cascade. Therefore, modification of the structure of curcumin could lead to analogs with enhanced activity. The library consisting of three series of curcumin analogs were used to examine the role of the enone functionality in aryl systems where the spacer is 7-carbons (as in curcumin), 5-carbons or 3-carbons in length. In addition, the importance of aryl ring substituents was assessed. The AP-1 activities of curcumin and analogs were determined by a cellular firefly luciferase assay. This assay utilized a commercially available cell line (Panomics 293-luc cellular assay) developed for screening inhibitors of AP-1. This cell line is stably transfected with a luciferase reporter controlled by an AP-1 dependent promoter. The cell is stimulated with phorbol ester which activates AP-1. AP-1 then binds to one of three promoter regions on the cells DNA leading to the production of a lucif
Drug: cycrimine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: cyproheptadine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.932
Drug: cyproheptadine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.951
Drug: cyproheptadine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.975
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: cyproheptadine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.855
Assay: DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
Drug: cyproheptadine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Drug: cyproheptadine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.39
Assay: Binding affinity towards Serotonin transporter using [3H]paroxetine as radioligand
Drug: cyproheptadine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.54
Assay: Binding affinity towards Norepinephrine transporter using [3H]nisoxitine as radioligand
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.229
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.419
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.812
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.652
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.8
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Drug: cyproheptadine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.4
Drug: cyproheptadine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.77
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: cyproheptadine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.097
Drug: cyproheptadine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.222
Action type: ANTAGONIST
Drug: cyproheptadine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.71
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: cyproheptadine
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.185
Drug: cyproheptadine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Drug: cyproheptadine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Drug: cyproheptadine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8
Drug: cyproheptadine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.66
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cyproheptadine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.559
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.886
Drug: cyproheptadine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.733
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: cyproheptadine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Drug: cyproheptadine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Drug: cyproheptadine
Target: Calmodulin (Cytosolic other)
Gene: CALM1|CALM2|CALM3
UniProt: P0DP23|P0DP24|P0DP25 (CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN)
Organism: Homo sapiens
Drug: cyproheptadine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.357
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.899
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: cyproheptadine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.62
Drug: cyproheptadine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 9
Assay: Potency against histamine H1 receptor on guinea pig ileum
Drug: cyproheptadine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.85
Assay: Binding affinity at dopamine D2 receptor by [3H]spiperone displacement.
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.91
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.8
Assay: Binding affinity against 5-hydroxytryptamine 2A receptor from rat forebrain using [3H]ketanserin as radioligand
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.3
Assay: Binding affinity towards 5-hydroxytryptamine 7 receptor
Drug: cyproheptadine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: Slc6a2
UniProt: O55192 (SC6A2_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.54
Assay: Binding affinity to Norepinephrine transporter using [3H]-nisoxatine as radioligand in stably transfected NIH3T3 cells
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P34968 (5HT2C_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.96
Assay: Binding affinity to 5-hydroxytryptamine 2C receptor using [3H]Mesulergine as radioligand in stably transfected NIH3T3 cells
Drug: cyproheptadine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61168 (DRD2_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.95
Assay: Binding affinity to Dopamine receptor D2 using [3H]spiperone as radioligand in stably transfected NIH3T3 cells
Drug: cyproheptadine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: Slc6a4
UniProt: Q60857 (SC6A4_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.39
Assay: Binding affinity to Serotonin transporter using [3H]-paroxetine as radioligand in stably transfected NIH3T3 cells
Drug: cyproheptadine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.9
Action type: ANTAGONIST