AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: choline theophyllinate
Target: Phosphodiesterase 4 (Enzyme)
Gene: PDE4A|PDE4B|PDE4C|PDE4D
UniProt: P27815|Q07343|Q08493|Q08499 (PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.25
Action type: INHIBITOR
Assay: Inhibition of c-AMP phosphodiesterase activity in guinea pig tracheal muscle
Drug: choline theophyllinate
Target: Adenosine A2b receptor (GPCR)
Gene: Adora2b
UniProt: P29276 (AA2BR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.82
Assay: Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
Drug: choline theophyllinate
Target: Adenosine receptor (GPCR)
Gene: Adora1|Adora3|Adora2b|Adora2a
UniProt: P25099|P28647|P29276|P30543 (AA1R_RAT|AA3R_RAT|AA2BR_RAT|AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.7
Assay: Antagonist binding of N6-cyclohexyl-[3H]-adenosine to rat testes
Drug: choline theophyllinate
Target: Adenosine A2 receptor (GPCR)
Gene: ADORA2A|ADORA2B
UniProt: P29274|P29275 (AA2AR_HUMAN|AA2BR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.85
Action type: ANTAGONIST
Assay: Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via adenosine A2 receptor in human platelet membranes.
Drug: choline theophyllinate
Target: Heart phosphodiesterase (Enzyme)
Gene: PDE3B|PDE1A|PDE1B
UniProt: E1BN64|P14100|Q01061 (E1BN64_BOVIN|PDE1A_BOVIN|PDE1B_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.04
Assay: Inhibition of bovine heart phosphodiesterase
Drug: choline theophyllinate
Target: Adenosine A2a receptor (GPCR)
Gene: ADORA2A
UniProt: P46616 (AA2AR_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 4.89
Assay: Antagonist binding of N6-cyclohexyl-[3H]-adenosine to guinea pig brain
Drug: cisplatin
Target: Sodium/potassium-transporting ATPase subunit alpha-2 (Ion channel)
Gene: ATP1A2
UniProt: D2WKD8 (AT1A2_PIG)
Organism: Sus scrofa
Activity: IC50 = 5.026
Assay: DRUGMATRIX: ATPase, Na+/K+ enzyme inhibition (substrate: ATP)
Drug: cisplatin
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.95
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: cisplatin
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.37
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: cisplatin
Target: Canalicular multispecific organic anion transporter 1 (Transporter)
Gene: ABCC2
UniProt: Q92887 (MRP2_HUMAN)
Organism: Homo sapiens
Drug: cisplatin
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.62
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: cisplatin
Target: Multidrug resistance-associated protein 6 (Transporter)
Gene: ABCC6
UniProt: O95255 (MRP6_HUMAN)
Organism: Homo sapiens
Drug: cisplatin
Target: Multidrug resistance-associated protein 5 (Transporter)
Gene: ABCC5
UniProt: O15440 (MRP5_HUMAN)
Organism: Homo sapiens
Drug: cisplatin
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.582
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: cisplatin
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.639
Assay: DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: cisplatin
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.321
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: cisplatin
Target: C-X-C chemokine receptor type 2 (GPCR)
Gene: CXCR2
UniProt: P25025 (CXCR2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.024
Assay: DRUGMATRIX: Chemokine CXCR2 (IL-8B) radioligand binding (ligand: [125I] IL-8)
Drug: cisplatin
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.029
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: cisplatin
Target: C-C chemokine receptor type 2 (GPCR)
Gene: CCR2
UniProt: P41597 (CCR2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.154
Assay: DRUGMATRIX: Chemokine CCR2B  radioligand binding (ligand: [125I] MCP-1)
Drug: cisplatin
Target: Mitogen-activated protein kinase 3 (Kinase)
Gene: MAPK3
UniProt: P27361 (MK03_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.335
Assay: DRUGMATRIX: Protein Serine/Threonine Kinase, ERK1 enzyme inhibition (substrate: Myelin Basic Protein)
Drug: cisplatin
Target: Melanocortin receptor 5 (GPCR)
Gene: MC5R
UniProt: P33032 (MC5R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.219
Assay: DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: clofenotane
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.74
Assay: Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)
Drug: clopenthixol
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.77
Assay: Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting
Drug: eltrombopag
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.16
Assay: Inhibition of human ERG channel tail current
Drug: eltrombopag
Target: Thrombopoietin receptor (Membrane receptor)
Gene: MPL
UniProt: P40238 (TPOR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.42
Action type: AGONIST
Drug: casopitant
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.53
Assay: Binding affinity to sigma 1 receptor
Drug: casopitant
Target: Substance-P receptor (GPCR)
Gene: TACR1
UniProt: P25103 (NK1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.9
Action type: ANTAGONIST
Assay: Displacement of [3H]GR205171 from human NK1 receptor in cortex homogenate by liquid scintillation counting
Drug: ceftobiprole medocaril
Target: MecA (Enzyme)
Gene: mecA
UniProt: Q7DHH4 (Q7DHH4_STAAU)
Organism: Staphylococcus aureus
Activity: IC50 = 5.49
Drug: plerixafor
Target: C-X-C chemokine receptor type 4 (GPCR)
Gene: CXCR4
UniProt: P61073 (CXCR4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.05
Action type: PARTIAL AGONIST
Assay: Displacement of [125I]12G5 antibody from human wild type CXCR4 expressed in COS7 cells
Drug: plerixafor
Target: C-C chemokine receptor type 2 (GPCR)
Gene: CCR2
UniProt: P41597 (CCR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 10.4
Assay: Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
Drug: plerixafor
Target: Stromal cell-derived factor 1 (Cytokine)
Gene: CXCL12
UniProt: P48061 (SDF1_HUMAN)
Organism: Homo sapiens
Drug: plerixafor
Target: C-C chemokine receptor type 4 (GPCR)
Gene: CCR4
UniProt: P51679 (CCR4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.19
Action type: ANTAGONIST
Drug: plerixafor
Target: C-X-C chemokine receptor type 4 (GPCR)
Gene: Cxcr4
UniProt: O08565 (CXCR4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.97
Assay: Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells
Drug: plerixafor
Target: Atypical chemokine receptor 3 (GPCR)
Gene: ACKR3
UniProt: P25106 (ACKR3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.85
Action type: AGONIST
Drug: dexchlorpheniramine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.118
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: dexchlorpheniramine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.157
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: dexchlorpheniramine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.886
Assay: DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)
Drug: dexchlorpheniramine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.308
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: dexchlorpheniramine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.977
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: dexchlorpheniramine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.915
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: dexchlorpheniramine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.677
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: dexchlorpheniramine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.14
Action type: ANTAGONIST
Assay: DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)
Drug: dexchlorpheniramine
Target: Histamine H2 receptor (GPCR)
Gene: HRH2
UniProt: P25021 (HRH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.085
Assay: DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)
Drug: dexchlorpheniramine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.478
Assay: DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: dexchlorpheniramine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.604
Assay: DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: dexchlorpheniramine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.262
Assay: DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: dexchlorpheniramine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.559
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: dexchlorpheniramine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.126
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: dexchlorpheniramine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.131
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: dexchlorpheniramine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.781
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: dexchlorpheniramine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.065
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: dexchlorpheniramine
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.931
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: diamorphine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.96
Assay: Dopamine receptor D2 affinity was tested in vitro against corpus striatum from rat brain membranes
Drug: diamorphine
Target: D(1A) dopamine receptor (GPCR)
Gene: Drd1
UniProt: P18901 (DRD1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.62
Assay: Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
Drug: diamorphine
Target: D(3) dopamine receptor (GPCR)
Gene: Drd3
UniProt: P19020 (DRD3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.44
Assay: Displacement of [3H]spiperone from rat recombinant dopamine D3 receptor expressed in SF9 cells
Drug: dibutylphthalate
Target: Transient receptor potential cation channel subfamily A member 1 (Ion channel)
Gene: TRPA1
UniProt: O75762 (TRPA1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.6
Action type: ACTIVATOR
Assay: Calcium imaging
Drug: dihydroergocryptine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.48
Action type: AGONIST
Assay: Biased for &beta;-arrestin signalling.
Drug: dihydroergocryptine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32305 (5HT7R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.5
Action type: ANTAGONIST
Drug: dihydroergocryptine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7
Action type: ANTAGONIST
Drug: colistin
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.824
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: colistin
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.018
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: colistin
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.652
Assay: DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: colistin
Target: Melanocortin receptor 4 (GPCR)
Gene: MC4R
UniProt: P32245 (MC4R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.092
Assay: DRUGMATRIX: Melanocortin MC4 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: colistin
Target: Melanocortin receptor 5 (GPCR)
Gene: MC5R
UniProt: P33032 (MC5R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.604
Assay: DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: colistin
Target: Melanocortin receptor 3 (GPCR)
Gene: MC3R
UniProt: P41968 (MC3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.775
Assay: DRUGMATRIX: Melanocortin MC3 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: bufylline
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.22
Action type: ANTAGONIST
Assay: Binding affinity for adenosine A2a receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2A cells
Drug: bufylline
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.22
Action type: ANTAGONIST
Assay: Binding affinity for adenosine A1 receptor by using as [3H]CPX iradioligand n membranes from Chinese hamster ovary cells
Drug: bufylline
Target: Adenosine receptor A2b (GPCR)
Gene: ADORA2B
UniProt: P29275 (AA2BR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.57
Action type: ANTAGONIST
Assay: Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
Drug: bufylline
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.85
Action type: ANTAGONIST
Assay: Binding affinity for adenosine A3 receptor by displacement of specific binding of [125I]AB-MECA in membranes from CHO-A3 cells
Drug: bufylline
Target: Alkaline phosphatase, tissue-nonspecific isozyme (Enzyme)
Gene: ALPL
UniProt: P05186 (PPBT_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.09
Assay: Inhibition of TNSALP
Drug: bufylline
Target: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Kinase)
Gene: PIK3CD
UniProt: O00329 (PK3CD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.12
Assay: Inhibition of PI3Kdelta (unknown origin)
Drug: bufylline
Target: Adenosine receptor A1 (GPCR)
Gene: Adora1
UniProt: P25099 (AA1R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.15
Assay: Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor
Drug: bufylline
Target: Adenosine receptor A2a (GPCR)
Gene: Adora2a
UniProt: P30543 (AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.17
Assay: Binding affinity at rat Adenosine A2A receptor by [3H]-CGS- 21680 displacement.
Drug: bufylline
Target: Uncharacterized protein (Enzyme)
Gene: PDE3B
UniProt: E1BN64 (E1BN64_BOVIN)
Organism: Bos taurus
Activity: Ki = 4.11
Assay: Inhibition of bovine heart phosphodiesterase
Drug: bufylline
Target: Adenosine receptor A3 (GPCR)
Gene: Adora3
UniProt: P28647 (AA3R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.07
Assay: Binding affinity to rat adenosine A3 receptor
Drug: bufylline
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P28190 (AA1R_BOVIN)
Organism: Bos taurus
Activity: Ki = 5.42
Assay: Binding affinity towards adenosine A1 receptor of bovine brain membrane using [3H]-CHA at 20 uM
Drug: bufylline
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P47745 (AA1R_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 5.01
Assay: Affinity against adenosine A1 receptor in the brain membranes by the displacement of [3H]CPX.
Drug: bufylline
Target: Adenosine A2 receptor (GPCR)
Gene: Adora2b|Adora2a
UniProt: P29276|P30543 (AA2BR_RAT|AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.88
Assay: Binding of Adenosine A2 receptor in whole rat brain membrane using [3H]CHA as a Radioligand
Drug: bufylline
Target: Phosphodiesterase 3 (Enzyme)
Gene: PDE3B|PDE3A
UniProt: Q13370|Q14432 (PDE3B_HUMAN|PDE3A_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2094125; PROTEIN FAMILY
Drug: bufylline
Target: Phosphodiesterase 4 (Enzyme)
Gene: PDE4A|PDE4B|PDE4C|PDE4D
UniProt: P27815|Q07343|Q08493|Q08499 (PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.25
Action type: INHIBITOR
Assay: Inhibition of c-AMP phosphodiesterase activity in guinea pig tracheal muscle
Drug: bufylline
Target: Adenosine A2b receptor (GPCR)
Gene: Adora2b
UniProt: P29276 (AA2BR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.82
Assay: Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
Drug: bufylline
Target: Adenosine receptor (GPCR)
Gene: Adora1|Adora3|Adora2b|Adora2a
UniProt: P25099|P28647|P29276|P30543 (AA1R_RAT|AA3R_RAT|AA2BR_RAT|AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.7
Assay: Antagonist binding of N6-cyclohexyl-[3H]-adenosine to rat testes
Drug: bufylline
Target: Adenosine A2 receptor (GPCR)
Gene: ADORA2A|ADORA2B
UniProt: P29274|P29275 (AA2AR_HUMAN|AA2BR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.85
Action type: ANTAGONIST
Assay: Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via adenosine A2 receptor in human platelet membranes.
Drug: bufylline
Target: Heart phosphodiesterase (Enzyme)
Gene: PDE3B|PDE1A|PDE1B
UniProt: E1BN64|P14100|Q01061 (E1BN64_BOVIN|PDE1A_BOVIN|PDE1B_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.04
Assay: Inhibition of bovine heart phosphodiesterase
Drug: bufylline
Target: Adenosine A2a receptor (GPCR)
Gene: ADORA2A
UniProt: P46616 (AA2AR_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 4.89
Assay: Antagonist binding of N6-cyclohexyl-[3H]-adenosine to guinea pig brain
Drug: calcitonin human
Target: Calcitonin receptor (GPCR)
Gene: CALCR
UniProt: P30988 (CALCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.81
Action type: AGONIST
Assay: IC50 values for peptides in competition for 125I-labeled salmon CT binding to COS-7 cells cotransfected with 100 ng of hCTR and 100 ng of RAMP.
Drug: calcitonin human
Target: Amylin receptor AMY1 (GPCR)
Gene: CALCR|RAMP1
UniProt: P30988|O60894 (CALCR_HUMAN|RAMP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.53
Action type: AGONIST
Assay: IC50 values for peptides in competition for 125I-labeled salmon CT binding to COS-7 cells cotransfected with 100 ng of hCTR and 100 ng of RAMP.
Drug: calcitonin human
Target: Amylin receptor AMY2 (GPCR)
Gene: CALCR|RAMP2
UniProt: P30988|O60895 (CALCR_HUMAN|RAMP2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.082
Action type: AGONIST
Assay: IC50 values for peptides in competition for 125I-labeled salmon CT binding to COS-7 cells cotransfected with 100 ng of hCTR and 100 ng of RAMP.
Drug: calcitonin human
Target: Amylin receptor AMY3 (GPCR)
Gene: CALCR|RAMP3
UniProt: P30988|O60896 (CALCR_HUMAN|RAMP3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.706
Action type: AGONIST
Assay: IC50 values for peptides in competition for 125I-labeled salmon CT binding to COS-7 cells cotransfected with 100 ng of hCTR and 100 ng of RAMP.
Drug: prednisolone sodium phosphate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action
Drug: clobetasol propionate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.179
Action type: AGONIST
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: clobetasol propionate
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: clobetasol propionate
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.07
Drug: clobetasol propionate
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.599
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: clobetasol propionate
Target: Cytochrome P450 3A5 (Enzyme)
Gene: CYP3A5
UniProt: P20815 (CP3A5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.68
Assay: Inhibition of CYP3A5 in doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for 24 hrs by LC-MS/MS analysis
Drug: clobetasol propionate
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.818
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: clobetasol propionate
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.5
Drug: clobetasol propionate
Target: Bile salt export pump (Transporter)
Gene: Abcb11
UniProt: O70127 (ABCBB_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.46
Drug: testosterone cypionate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL1871; SINGLE PROTEIN
Drug: hydrocortisone succinate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL2034; SINGLE PROTEIN