AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: oxybutynin
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.44
Assay: Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug: oxybutynin
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.85
Assay: Displacement of [3H]N-methylscopolamine from human muscarinic M5 receptor expressed in CHO cells after 120 mins by scintillation counting
Drug: oxybutynin
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.168
Assay: DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: oxybutynin
Target: Cytochrome P450 2C19 (Enzyme)
Gene: CYP2C19
UniProt: P33261 (CP2CJ_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.222
Assay: DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: oxybutynin
Target: Membrane-associated progesterone receptor component 1 (Membrane receptor)
Gene: Pgrmc1
UniProt: P70580 (PGRC1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.086
Assay: DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
Drug: oxybutynin
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.16
Assay: Affinity for rat Muscarinic acetylcholine receptor M2
Drug: oxybutynin
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.23
Assay: Binding affinity for rat cortex muscarinic acetylcholine receptor M1 using [3H]pirenzepine
Drug: oxybutynin
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: Chrm3
UniProt: P08483 (ACM3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.02
Assay: Affinity for rat Muscarinic acetylcholine receptor M3
Drug: oxybutynin
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: ANTAGONIST
Assay: Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M1 receptor expressed in Sf9 cells
Drug: oxybutynin
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.11
Action type: ANTAGONIST
Assay: Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
Drug: oxycodone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.796
Action type: AGONIST
Drug: oxycodone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.8
Assay: Agonist activity at human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay
Drug: oxycodone
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.4
Assay: Agonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay
Drug: oxycodone
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.36
Assay: Displacement of [3H]DAMGO from mu opioid receptor of rat brain membranes
Drug: oxycodone
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P42866 (OPRM_MOUSE)
Organism: Mus musculus
Activity: EC50 = 6.8
Assay: Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay
Drug: oxycodone
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P33533 (OPRD_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.96
Assay: Displacement of [3H[Ile5,6]-deltorphin II from delta opioid receptor of rat brain membranes
Drug: oxycodone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41144 (OPRK_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 6.49
Assay: Displacement of [3H]HS-665 from KOR in guinea pig brain membranes after 60 mins by liquid scintillation analysis
Drug: oxycodone
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: IC50 = 4.12
Assay: Inhibition of electric eel AChE by Ellman's method
Drug: oxycodone
Target: Kappa-type opioid receptor (GPCR)
Gene: Oprk1
UniProt: P34975 (OPRK_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.58
Assay: Displacement of [3H]U-69593 from kappa opioid receptor of rat brain membranes
Drug: oxycodone
Target: Kappa-type opioid receptor (GPCR)
Gene: Oprk1
UniProt: P33534 (OPRK_MOUSE)
Organism: Mus musculus
Activity: EC50 = 4.8
Assay: Agonist activity at mouse KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay
Drug: oxymetazoline
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.54
Action type: AGONIST
Assay: Displacement of [125I]Clonidine from adrenergic alpha2A receptor (unknown origin)
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.493
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.59
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.83
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.8
Action type: AGONIST
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.111
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: oxymetazoline
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.342
Assay: DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: oxymetazoline
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.019
Assay: DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine)
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.52
Assay: Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.4
Assay: Binding affinity towards human 5-hydroxytryptamine 1D receptor using [3H]5-HT trifluoroacetate as radioligand
Drug: oxymetazoline
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: AGONIST
Assay: Displacement of [125I]Clonidine from adrenergic alpha2C receptor (unknown origin)
Drug: oxymetazoline
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.699
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: oxymetazoline
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: AGONIST
Drug: oxymetazoline
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.5
Action type: AGONIST
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.379
Drug: oxymetazoline
Target: Nischarin (Membrane receptor)
Gene: NISCH
UniProt: Q9Y2I1 (NISCH_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.21
Assay: Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR
Drug: oxymetazoline
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.162
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.041
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: oxymetazoline
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.19
Drug: oxymetazoline
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: Adra1d
UniProt: P23944 (ADA1D_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.48
Drug: oxymetazoline
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.25
Drug: oxymetazoline
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.88
Drug: oxymetazoline
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P18871 (ADA2A_PIG)
Organism: Sus scrofa
Activity: Ki = 7.68
Assay: Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in porcine alpha2-clone
Drug: oxymetazoline
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: Q28838 (ADA2A_BOVIN)
Organism: Bos taurus
Activity: Ki = 8.82
Assay: Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in bovine pineal
Drug: oxymetazoline
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P18841 (ADA1B_MESAU)
Organism: Mesocricetus auratus
Activity: Ki = 6.69
Drug: oxymetazoline
Target: Adrenergic receptor alpha-2 (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P19328|P22086|P22909 (ADA2B_RAT|ADA2C_RAT|ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.72
Assay: The ability to displace [3H]clonidine from the Alpha-2 adrenergic receptor was determined in rat brain membrane
Drug: oxymetazoline
Target: Alpha-2 adrenergic receptor (GPCR)
Gene: Adra2b|Adra2c|Adra2a
UniProt: P30545|Q01337|Q01338 (ADA2B_MOUSE|ADA2C_MOUSE|ADA2A_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.48
Assay: Compound was evaluated for inhibition of binding of [3H]MK-91 to Alpha-2 adrenergic receptor in mouse Malpha2-10H clone
Drug: oxymetazoline
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.2
Action type: AGONIST
Drug: oxymetazoline
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.2
Action type: AGONIST
Drug: oxymetholone
Target: Estrogen receptor (Nuclear hormone receptor)
Gene: ESR1
UniProt: P03372 (ESR1_HUMAN)
Organism: Homo sapiens
Drug: oxymetholone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: oxymetholone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.863
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: oxymorphone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.444
Action type: AGONIST
Drug: oxymorphone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41145 (OPRK_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.83
Action type: AGONIST
Drug: oxymorphone
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.3
Action type: AGONIST
Assay: Inhibitory binding constant in guinea pig brain homogenate was reported at Opioid receptor delta 1 at a a temperature 25 degree Celsius labeled with [3H](D-Ala2-D-Leu5)-enkephalin (0.7 nM)
Drug: oxymorphone
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P33535 (OPRM_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.01
Assay: Inhibition of [3H]DAMGO binding to opioid receptor mu from rat brain membranes
Drug: oxymorphone
Target: Mu-type opioid receptor (GPCR)
Gene: Oprm1
UniProt: P42866 (OPRM_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.3
Assay: Displacement of [3H]-DAMGO from mouse MOR expressed in HEK293 cells
Drug: oxymorphone
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P97266 (OPRM_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 9.27
Assay: Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain homogenate by scintillation counting
Drug: oxymorphone
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P32300 (OPRD_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.21
Assay: Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells
Drug: oxymorphone
Target: Delta-type opioid receptor (GPCR)
Gene: Oprd1
UniProt: P33533 (OPRD_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.09
Assay: Inhibition of [3H][Ile5,6]deltorphin II binding to opioid receptor delta from rat brain membranes
Drug: oxymorphone
Target: Kappa-type opioid receptor (GPCR)
Gene: OPRK1
UniProt: P41144 (OPRK_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 7.24
Assay: Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum homogenate by scintillation counting
Drug: oxymorphone
Target: Kappa-type opioid receptor (GPCR)
Gene: Oprk1
UniProt: P34975 (OPRK_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.02
Assay: Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells
Drug: oxymorphone
Target: Opioid receptor (GPCR)
Gene: Oprd1|Oprm1|Oprk1|Sigmar1
UniProt: P33533|P33535|P34975|Q9R0C9 (OPRD_RAT|OPRM_RAT|OPRK_RAT|SGMR1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 10.89
Assay: Concentration for 50% inhibition of [3H]naloxone (1 M) binding to opioid receptor in rat brain membrane was determined in the absence of NaCl
Drug: oxymorphone
Target: Opioid receptors; mu and delta (GPCR)
Gene: Oprd1|Oprm1
UniProt: P32300|P42866 (OPRD_MOUSE|OPRM_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.33
Assay: Displacement of [3H]-DAMGO from mouse MOR/DOR expressed in HEK293 cells
Drug: oxyphenbutazone
Target: fMet-Leu-Phe receptor (GPCR)
Gene: FPR1
UniProt: P21462 (FPR1_HUMAN)
Organism: Homo sapiens
Drug: oxyphenbutazone
Target: Prostacyclin synthase (Enzyme)
Gene: PTGIS
UniProt: Q16647 (PTGIS_HUMAN)
Organism: Homo sapiens
Drug: oxyphenbutazone
Target: Cyclooxygenase (Enzyme)
Gene: PTGS1|PTGS2
UniProt: P23219|P35354 (PGH1_HUMAN|PGH2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2094253; PROTEIN FAMILY
Drug: oxyphenbutazone
Target: Nicotinate phosphoribosyltransferase (Enzyme)
Gene: NAPRT
UniProt: Q6XQN6 (PNCB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.52
Assay: Inhibition of NAPRT (unknown origin)
Drug: oxyphenonium
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: oxyphenonium
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: oxyphenonium
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.84
Action type: ANTAGONIST
Drug: oxytetracycline
Target: 30S ribosomal protein S4 (Ribosomal protein)
Gene: rpsD
UniProt: P0A7V8 (RS4_ECOLI)
Organism: Escherichia coli (strain K12)
Drug: oxytetracycline
Target: 30S ribosomal protein S9 (Ribosomal protein)
Gene: rpsI
UniProt: P0A7X3 (RS9_ECOLI)
Organism: Escherichia coli (strain K12)
Drug: oxytocin
Target: Vasopressin V1a receptor (GPCR)
Gene: AVPR1A
UniProt: P37288 (V1AR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.91
Drug: oxytocin
Target: Vasopressin V1b receptor (GPCR)
Gene: AVPR1B
UniProt: P47901 (V1BR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.35
Drug: oxytocin
Target: Vasopressin V2 receptor (GPCR)
Gene: AVPR2
UniProt: P30518 (V2R_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.1
Drug: oxytocin
Target: Oxytocin receptor (GPCR)
Gene: OXTR
UniProt: P30559 (OXYR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.1
Action type: AGONIST
Assay: Binding affinity for human oxytocin receptor
Drug: oxytocin
Target: Oxytocin-neurophysin 1 (Secreted)
Gene: OXT
UniProt: P01178 (NEU1_HUMAN)
Organism: Homo sapiens
Drug: oxytocin
Target: Oxytocin receptor (GPCR)
Gene: Oxtr
UniProt: P70536 (OXYR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.05
Assay: Binding affinity against oxytocin receptor in rat uterus
Drug: oxytocin
Target: Vasopressin V2 receptor (GPCR)
Gene: Avpr2
UniProt: Q00788 (V2R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.21
Assay: Binding affinity against Vasopressin receptor in rat liver
Drug: oxytocin
Target: Vasopressin V1a receptor (GPCR)
Gene: Avpr1a
UniProt: P30560 (V1AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.1
Action type: AGONIST
Drug: ozagrel
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.96
Assay: Inhibitory activity against human thromboxane synthetase
Drug: ozagrel
Target: Thromboxane-A synthase (Enzyme)
Gene: Tbxas1
UniProt: P49430 (THAS_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.7
Assay: Tested in vitro against TXA2 synthetase inhibitory activity in rat platelet
Drug: paclitaxel
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.59
Assay: Inhibition of MDR1 (unknown origin) transfected in human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay
Drug: paclitaxel
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.3
Action type: AGONIST
Drug: paclitaxel
Target: Delta-type opioid receptor (GPCR)
Gene: OPRD1
UniProt: P41143 (OPRD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.829
Assay: DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)
Drug: paclitaxel
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Drug: paclitaxel
Target: Multidrug resistance-associated protein 7 (Transporter)
Gene: ABCC10
UniProt: Q5T3U5 (MRP7_HUMAN)
Organism: Homo sapiens
Drug: paclitaxel
Target: Tubulin beta chain (Structural)
Gene: TUBB
UniProt: P07437 (TBB5_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.05
Action type: INHIBITOR
Drug: paclitaxel
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.621
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: paclitaxel
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.954
Assay: DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: paclitaxel
Target: Cholecystokinin receptor type A (GPCR)
Gene: CCKAR
UniProt: P32238 (CCKAR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.643
Assay: DRUGMATRIX: Cholecystokinin CCKA radioligand binding (ligand: [3H] L-364,718)
Drug: paclitaxel
Target: Substance-K receptor (GPCR)
Gene: TACR2
UniProt: P21452 (NK2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.69
Assay: DRUGMATRIX: Tachykinin NK2  radioligand binding (ligand: [3H] SR-48968)
Drug: paclitaxel
Target: Melanocortin receptor 5 (GPCR)
Gene: MC5R
UniProt: P33032 (MC5R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.794
Assay: DRUGMATRIX: Melanocortin MC5 radioligand binding (ligand: [125I] NDP-alpha-MSH)
Drug: paclitaxel
Target: Botulinum neurotoxin type A (Enzyme)
Gene: botA
UniProt: P10845 (BXA1_CLOBO)
Organism: Clostridium botulinum
Activity: IC50 = 5.28
Assay: Inhibition of Clostridium botulinum recombinant neurotoxin A light chain using SNAPtide as substrate after 1 hr by FRET assay
Drug: paclitaxel
Target: Tyrosine-protein kinase Mer (Kinase)
Gene: MERTK
UniProt: Q12866 (MERTK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.31
Assay: Inhibition of MERTK (unknown origin) using EFPIYDFLPAKKK-CONH2 as substrate and ATP after 180 mins by microfluidic capillary electrophoresis method
Drug: paclitaxel
Target: Tubulin beta-3 chain (Structural)
Gene: TUBB3
UniProt: Q13509 (TBB3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.11
Assay: Inhibition of beta3 tubulin overexpressed in human HeLa cells after 48 hrs by SRB assay
Drug: paclitaxel
Target: Nucleotide-binding oligomerization domain-containing protein 2 (Cytosolic other)
Gene: NOD2
UniProt: Q9HC29 (NOD2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Assay: Inhibition of MDP-induced human NOD2 signaling expressed in HEK-Blue cells preincubated for 3 hrs followed by MDP-stimulation for 20 hrs by spectrophotometry based SEAP reporter gene assay
Drug: paclitaxel
Target: Tubulin beta (Tumour-associated antigen)
Gene: TUBB|TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB6|TUBB8
UniProt: P07437|Q9H4B7|Q13885|Q9BVA1|Q13509|P04350|P68371|Q9BUF5|Q3ZCM7 (TBB5_HUMAN|TBB1_HUMAN|TBB2A_HUMAN|TBB2B_HUMAN|TBB3_HUMAN|TBB4A_HUMAN|TBB4B_HUMAN|TBB6_HUMAN|TBB8_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.05
Action type: INHIBITOR
Drug: palmidrol
Target: Cannabinoid receptor 1 (GPCR)
Gene: CNR1
UniProt: P21554 (CNR1_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: palmidrol
Target: Cannabinoid receptor 2 (GPCR)
Gene: CNR2
UniProt: P34972 (CNR2_HUMAN)
Organism: Homo sapiens
Activity: Ki  5.301
Drug: palmidrol
Target: Fatty-acid amide hydrolase 1 (Enzyme)
Gene: Faah
UniProt: P97612 (FAAH1_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.3
Assay: Inhibition of rat recombinant FAAH assessed as [3H]AEA hydrolysis
Drug: palmidrol
Target: G-protein coupled receptor 55 (GPCR)
Gene: GPR55
UniProt: Q9Y2T6 (GPR55_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.4
Action type: AGONIST
Drug: palonosetron
Target: 5-hydroxytryptamine receptor 3A (Ion channel)
Gene: HTR3A
UniProt: P46098 (5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.5
Action type: ANTAGONIST
Assay: Binding affinity to 5HT3A receptor
Drug: palonosetron
Target: Serotonin 3 receptor (5HT3) (Ion channel)
Gene: HTR3B|HTR3A
UniProt: O95264|P46098 (5HT3B_HUMAN|5HT3A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 9.74
Assay: Binding affinity to human wild type 5-HT3A/5-HT3B receptor expressed in HEK293 cells after 24 hrs by liquid scintillation counting analysis
Drug: pamabrom
Target: Adenosine receptor A1 (GPCR)
Gene: Adora1
UniProt: P25099 (AA1R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.99
Assay: Binding affinity for adenosine A1 receptor from rat brain membranes using [3H]PIA as radioligand
Drug: pamidronic acid
Target: Farnesyl pyrophosphate synthase (Enzyme)
Gene: FDPS
UniProt: P14324 (FPPS_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.25
Action type: INHIBITOR
Assay: Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins
Drug: pamidronic acid
Target: Farnesyl pyrophosphate synthase (Enzyme)
UniProt: Q0GKD7 (Q0GKD7_LEIDO)
Organism: Leishmania donovani
Activity: Ki = 6.72
Assay: Binding affinity towards Farnesyl diphosphate synthase from leishmania major
Drug: pamidronic acid
Target: Hypoxanthine-guanine phosphoribosyltransferase (Enzyme)
Gene: HGPRT
UniProt: Q07010 (HPRT_TRYBB)
Organism: Trypanosoma brucei brucei
Activity: Ki = 4.3
Assay: Inhibition of hypoxanthine-guanine phosphoribosyltransferase (TcHPRT)