AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: dimetindene
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.1
Drug: dimethyltubocurarinium
Target: Acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNB1|CHRND
UniProt: P02708|P11230|Q07001 (ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.745
Action type: ANTAGONIST
Drug: dimethyltubocurarinium
Target: Neuronal acetylcholine receptor; alpha2/beta2 (Ion channel)
Gene: CHRNB2|CHRNA2
UniProt: P17787|Q15822 (ACHB2_HUMAN|ACHA2_HUMAN)
Organism: Homo sapiens
Drug: dioxyline
Target: Methionine aminopeptidase 2 (Enzyme)
Gene: METAP2
UniProt: P50579 (MAP2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.46
Assay: Inhibition of human MetAP2 expressed in baculovirus infected Sf9 cells
Drug: dioxyline
Target: Methionine aminopeptidase 1 (Enzyme)
Gene: METAP1
UniProt: P53582 (MAP11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.37
Assay: Inhibition of human MetAP1
Drug: dinoprost
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: PTGER1
UniProt: P34995 (PE2R1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.66
Assay: In vitro binding at EP1 human prostaglandin receptor using [3H]PGE-2 as radioligand
Drug: dinoprost
Target: Prostaglandin D2 receptor 2 (GPCR)
Gene: PTGDR2
UniProt: Q9Y5Y4 (PD2R2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: AGONIST
Drug: dinoprost
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: PTGER3
UniProt: P43115 (PE2R3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.96
Assay: In vitro binding at EP3 human prostaglandin receptor using [3H]PGE-2 as radioligand
Drug: dinoprost
Target: Thromboxane A2 receptor (GPCR)
Gene: TBXA2R
UniProt: P21731 (TA2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.1
Action type: AGONIST
Drug: dinoprost
Target: Prostaglandin E2 receptor EP2 subtype (GPCR)
Gene: PTGER2
UniProt: P43116 (PE2R2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Action type: AGONIST
Drug: dinoprost
Target: Prostaglandin E2 receptor EP4 subtype (GPCR)
Gene: PTGER4
UniProt: P35408 (PE2R4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.38
Assay: Affinity for Prostanoid EP4 receptor expressed in CHO cells
Drug: dinoprost
Target: Prostaglandin D2 receptor (GPCR)
Gene: PTGDR
UniProt: Q13258 (PD2R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.35
Assay: Affinity for human Prostaglandin D2 receptor expressed in HEK293 cells
Drug: dinoprost
Target: Prostaglandin F2-alpha receptor (GPCR)
Gene: PTGFR
UniProt: P43088 (PF2R_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.4
Action type: AGONIST
Assay: GRAC: human FP probe
Drug: dinoprost
Target: Prostaglandin F2-alpha receptor (GPCR)
Gene: PTGFR
UniProt: P37289 (PF2R_BOVIN)
Organism: Bos taurus
Activity: Ki = 6.89
Assay: Binding affinity for Prostanoid FP receptor of bovine corpus luteum
Drug: dinoprost
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: Ptger1
UniProt: P35375 (PE2R1_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.9
Action type: AGONIST
Drug: dinoprost
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: Ptger3
UniProt: P30557 (PE2R3_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.12
Action type: AGONIST
Drug: dinoprost
Target: Prostaglandin F2-alpha receptor (GPCR)
Gene: Ptgfr
UniProt: P43117 (PF2R_MOUSE)
Organism: Mus musculus
Activity: EC50 = 7.9
Assay: Agonist activity at FP receptor in mouse 3T3 fibroblast cells assessed as intracellular calcium mobilization by FLIPR
Drug: dinoprost
Target: Prostaglandin E2 receptor EP2 subtype (GPCR)
Gene: Ptger2
UniProt: Q62928 (PE2R2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.6
Action type: AGONIST
Drug: dinoprost
Target: Prostaglandin E2 receptor EP4 subtype (GPCR)
Gene: Ptger4
UniProt: P43114 (PE2R4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.2
Action type: AGONIST
Drug: dinoprost
Target: Prostaglandin D2 receptor 2 (GPCR)
Gene: Ptgdr2
UniProt: Q9Z2J6 (PD2R2_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.2
Action type: AGONIST
Drug: dinoprost
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: Ptger3
UniProt: P34980 (PE2R3_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 8.38
Action type: AGONIST
Drug: dinoprost
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: Ptger1
UniProt: P70597 (PE2R1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.4
Action type: AGONIST
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: PTGER1
UniProt: P34995 (PE2R1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.04
Action type: AGONIST
Assay: Displacement of [3H]PGE2 from human EP1 receptor expressed in HEK293 cells
Drug: dinoprostone
Target: Prostaglandin D2 receptor 2 (GPCR)
Gene: PTGDR2
UniProt: Q9Y5Y4 (PD2R2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.3
Action type: AGONIST
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: PTGER3
UniProt: P43115 (PE2R3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.48
Action type: AGONIST
Assay: Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells
Drug: dinoprostone
Target: Prostacyclin receptor (GPCR)
Gene: PTGIR
UniProt: P43119 (PI2R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.59
Assay: Agonist activity at prostanoid IP receptor (unknown origin) by functional assay
Drug: dinoprostone
Target: Thromboxane A2 receptor (GPCR)
Gene: TBXA2R
UniProt: P21731 (TA2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.5
Action type: AGONIST
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP2 subtype (GPCR)
Gene: PTGER2
UniProt: P43116 (PE2R2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.77
Action type: AGONIST
Assay: Binding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP4 subtype (GPCR)
Gene: PTGER4
UniProt: P35408 (PE2R4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.77
Action type: AGONIST
Assay: Binding affinity to human prostanoid EP4 receptor by radioligand displacement assay
Drug: dinoprostone
Target: Prostaglandin D2 receptor (GPCR)
Gene: PTGDR
UniProt: Q13258 (PD2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Action type: AGONIST
Drug: dinoprostone
Target: Prostaglandin F2-alpha receptor (GPCR)
Gene: PTGFR
UniProt: P43088 (PF2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Action type: AGONIST
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: Ptger1
UniProt: P35375 (PE2R1_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.22
Assay: Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP2 subtype (GPCR)
Gene: Ptger2
UniProt: Q62053 (PE2R2_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.66
Assay: Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: Ptger3
UniProt: P30557 (PE2R3_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.3
Assay: Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP4 subtype (GPCR)
Gene: Ptger4
UniProt: P32240 (PE2R4_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.51
Assay: Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug: dinoprostone
Target: Solute carrier family 22 member 6 (Transporter)
Gene: Slc22a6
UniProt: Q8VC69 (S22A6_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.47
Assay: Inhibition of mouse Oat1-mediated [3H]PAH uptake in Xenopus oocytes after 1 hr
Drug: dinoprostone
Target: Solute carrier family 22 member 20 (Transporter)
Gene: Slc22a20
UniProt: Q80UJ1 (S22AK_MOUSE)
Organism: Mus musculus
Activity: Ki = 4.74
Assay: Inhibition of mouse Oat6-mediated [3H]ES uptake in Xenopus oocytes after 1 hr
Drug: dinoprostone
Target: Prostaglandin F2-alpha receptor (GPCR)
Gene: Ptgfr
UniProt: P43117 (PF2R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7
Action type: AGONIST
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP2 subtype (GPCR)
Gene: Ptger2
UniProt: Q62928 (PE2R2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.28
Assay: Inhibition of rat EP2 receptor expressed in HEK293 cells
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP4 subtype (GPCR)
Gene: Ptger4
UniProt: P43114 (PE2R4_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.68
Assay: Inhibition of rat EP4 receptor expressed in HEK293 cells
Drug: dinoprostone
Target: Cation channel sperm-associated protein 1 (Ion channel)
Gene: CATSPER1
UniProt: Q8NEC5 (CTSR1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.3
Action type: ACTIVATOR
Assay: Patch clamp electrophysiology
Drug: dinoprostone
Target: Cation channel sperm-associated protein 2 (Ion channel)
Gene: CATSPER2
UniProt: Q96P56 (CTSR2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.3
Action type: ACTIVATOR
Assay: Patch clamp electrophysiology.
Drug: dinoprostone
Target: Cation channel sperm-associated protein 3 (Ion channel)
Gene: CATSPER3
UniProt: Q86XQ3 (CTSR3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.3
Action type: ACTIVATOR
Assay: Patch clamp electrophysiology.
Drug: dinoprostone
Target: Cation channel sperm-associated protein 4 (Ion channel)
Gene: CATSPER4
UniProt: Q7RTX7 (CTSR4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 6.3
Action type: ACTIVATOR
Assay: Patch clamp electrophysiology.
Drug: dinoprostone
Target: Prostaglandin D2 receptor 2 (GPCR)
Gene: Ptgdr2
UniProt: Q9Z2J6 (PD2R2_MOUSE)
Organism: Mus musculus
Activity: Ki = 5.5
Action type: AGONIST
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP3 subtype (GPCR)
Gene: Ptger3
UniProt: P34980 (PE2R3_RAT)
Organism: Rattus norvegicus
Activity: EC50 = 9.39
Action type: AGONIST
Drug: dinoprostone
Target: Prostaglandin E2 receptor EP1 subtype (GPCR)
Gene: Ptger1
UniProt: P70597 (PE2R1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.7
Action type: AGONIST
Drug: diphemanil
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL216; SINGLE PROTEIN
Drug: diphemanil
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: diphenhydramine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.59
Assay: Inhibition of human ERG
Drug: diphenhydramine
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.018
Drug: diphenhydramine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.432
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
Drug: diphenhydramine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.148
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: diphenhydramine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.29
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: diphenhydramine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.81
Action type: ANTAGONIST
Drug: diphenhydramine
Target: Histamine H4 receptor (GPCR)
Gene: HRH4
UniProt: Q9H3N8 (HRH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.37
Assay: Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting
Drug: diphenhydramine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7
Drug: diphenhydramine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.921
Drug: diphenhydramine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.64
Drug: diphenhydramine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.951
Drug: diphenhydramine
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.585
Drug: diphenhydramine
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.932
Drug: diphenhydramine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P31389 (HRH1_CAVPO)
Organism: Cavia porcellus
Activity: IC50 = 9
Assay: Antihistaminic activity against Histamine H1 receptor was measured on isolated terminal part of guinea pig ileum
Drug: diphenhydramine
Target: Solute carrier family 22 member 2 (Transporter)
Gene: SLC22A2
UniProt: O15244 (S22A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.678
Drug: diphenhydramine
Target: Sodium channel alpha subunits; brain (Types I, II, III) (Ion channel)
Gene: SCN1A|SCN2A|SCN3A
UniProt: P35498|Q99250|Q9NY46 (SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.22
Assay: Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex
Drug: diphenhydramine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.42
Drug: diphenhydramine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.658
Drug: diphenoxylate
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.167
Action type: AGONIST
Drug: diphenoxylate
Target: Potassium voltage-gated channel subfamily A member 3 (Ion channel)
Gene: KCNA3
UniProt: P22001 (KCNA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.3
Assay: Inhibition of Kv1.3 expressed in mouse L929 cells exposed to depolarizing step pulses from -80 mV to +40 mV by whole cell patch clamp method
Drug: diphenylpyraline
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.076
Action type: ANTAGONIST
Drug: diphenylpyraline
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.699
Drug: diphenylpyraline
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.377
Drug: diphenylpyraline
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Drug: diphenylpyraline
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 6.38
Assay: Displacement of [125I]RTI-55 dopamine transporter binding in rat striatal membrane
Drug: dipivefrine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: dipivefrine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: dipivefrine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: diprafenone
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Drug: diprafenone
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Drug: diprafenone
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Drug: dipyridamole
Target: Sodium/nucleoside cotransporter 1 (Transporter)
Gene: SLC28A1
UniProt: O00337 (S28A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.538
Action type: INHIBITOR
Assay: DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
Drug: dipyridamole
Target: cGMP-specific 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE5A
UniProt: O76074 (PDE5A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.28
Action type: INHIBITOR
Assay: Inhibitory activity against cyclic GMP-phosphodiesterase (PDE V) isolated from porcine aorta.
Drug: dipyridamole
Target: Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (Enzyme)
Gene: PDE11A
UniProt: Q9HCR9 (PDE11_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Assay: Inhibition of human phosphodiesterase 11
Drug: dipyridamole
Target: cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Enzyme)
Gene: PDE10A
UniProt: Q9Y233 (PDE10_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Action type: INHIBITOR
Assay: Inhibitory activity against phosphodiesterase 10
Drug: dipyridamole
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Enzyme)
Gene: PDE4A
UniProt: P27815 (PDE4A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.802
Action type: INHIBITOR
Assay: DRUGMATRIX: Phosphodiesterase PDE4 enzyme inhibition (substrate: [3H]cAMP + cAMP)
Drug: dipyridamole
Target: Equilibrative nucleoside transporter 1 (Transporter)
Gene: SLC29A1
UniProt: Q99808 (S29A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.5
Action type: INHIBITOR
Assay: GRAC: human ENT1 selective inhibitor
Drug: dipyridamole
Target: High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B (Enzyme)
Gene: PDE8B
UniProt: O95263 (PDE8B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Action type: INHIBITOR
Drug: dipyridamole
Target: cGMP-dependent 3',5'-cyclic phosphodiesterase (Enzyme)
Gene: PDE2A
UniProt: O00408 (PDE2A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.49
Action type: INHIBITOR
Assay: Inhibition of phosphodiesterase 2 (PDE2) from porcine platelets, range 2.54-4.14
Drug: dipyridamole
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 7B (Enzyme)
Gene: PDE7B
UniProt: Q9NP56 (PDE7B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: INHIBITOR
Assay: GRAC: human PDE7B selective inhibitor
Drug: dipyridamole
Target: High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A (Enzyme)
Gene: PDE8A
UniProt: O60658 (PDE8A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.1
Action type: INHIBITOR
Assay: GRAC: human PDE8A selective inhibitor
Drug: dipyridamole
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 5.158
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: dipyridamole
Target: Cyclic nucleotide phosphodiesterase PDE3A (Enzyme)
UniProt: Q9XSW7 (Q9XSW7_PIG)
Organism: Sus scrofa
Activity: IC50 = 4.36
Assay: Inhibition of phosphodiesterase 3 (PDE3) from porcine platelets, range 31.8-60.7
Drug: dipyridamole
Target: Cyclic AMP-specific phosphodiesterase SSPDE4A1A (Enzyme)
Gene: PDE4A
UniProt: O77823 (O77823_PIG)
Organism: Sus scrofa
Activity: IC50 = 5.28
Assay: Inhibition of phosphodiesterase 4 (PDE4) from porcine liver, range 0.058-7.78
Drug: dipyridamole
Target: Phosphodiesterase 3 (Enzyme)
Gene: PDE3B|PDE3A
UniProt: Q13370|Q14432 (PDE3B_HUMAN|PDE3A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.37
Action type: INHIBITOR
Assay: Inhibition of low Km cyclic cAMP phosphodiesterase PDE III of guinea pig ventricle
Drug: dipyridamole
Target: Phosphodiesterase 7 (Enzyme)
Gene: PDE7A|PDE7B
UniProt: Q13946|Q9NP56 (PDE7A_HUMAN|PDE7B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.22
Action type: INHIBITOR
Assay: Inhibition of human phosphodiesterase 7
Drug: dipyridamole
Target: Phosphodiesterase 6 (Enzyme)
Gene: PDE6D|PDE6A|PDE6G|PDE6B|PDE6C|PDE6H
UniProt: O43924|P16499|P18545|P35913|P51160|Q13956 (PDE6D_HUMAN|PDE6A_HUMAN|CNRG_HUMAN|PDE6B_HUMAN|PDE6C_HUMAN|CNCG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.9
Action type: INHIBITOR
Assay: Inhibition of human phosphodiesterase 6
Drug: dipyridamole
Target: Phosphodiesterase 1 (Enzyme)
Gene: PDE1A|PDE1B|PDE1C
UniProt: P54750|Q01064|Q14123 (PDE1A_HUMAN|PDE1B_HUMAN|PDE1C_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.35
Action type: INHIBITOR
Assay: Inhibition of [Ca(2+)]/calmodulin dependent phosphodiesterase PDE 1 of guinea pig ventricle
Drug: dipyridamole
Target: Equilibrative nucleoside transporter 4 (Transporter)
Gene: SLC29A4
UniProt: Q7RTT9 (S29A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.9
Action type: INHIBITOR
Drug: dipyridamole
Target: Protein prune homolog (Enzyme)
Gene: PRUNE
UniProt: Q86TP1 (PRUNE_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.11
Assay: Inhibition of human prune assessed as reduction of cAMP-phosphodiesterase activity
Drug: dipyridamole
Target: ORF 73 (Unclassified)
UniProt: O40947 (O40947_HHV8)
Organism: Human herpesvirus 8
Activity: AC50 = 5.05
Assay: Active
Drug: dipyridamole
Target: Replicase polyprotein 1ab (Enzyme)
Gene: REP
UniProt: P0DTD1 (R1AB_SARS2)
Organism: Severe acute respiratory syndrome coronavirus 2 (2019-nCoV) (SARS-CoV-2)
Activity: IC50 = 6.26
Action type: INHIBITOR
Drug: disopyramide
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: disopyramide
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.036
Drug: disopyramide
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.569
Drug: disopyramide
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Drug: disopyramide
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Drug: disopyramide
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Drug: disopyramide
Target: G protein-activated inward rectifier potassium channel 4 (Ion channel)
Gene: KCNJ5
UniProt: P48544 (KCNJ5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.921
Drug: disopyramide
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.09
Assay: Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Drug: disopyramide
Target: Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Ion channel)
Gene: HCN4
UniProt: Q9Y3Q4 (HCN4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 3.604
Drug: distigmine
Target: Acetylcholinesterase (Enzyme)
Gene: ACHE
UniProt: P22303 (ACES_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action
Drug: disulfiram
Target: Sodium/nucleoside cotransporter 1 (Transporter)
Gene: SLC28A1
UniProt: O00337 (S28A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.237
Assay: DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
Drug: disulfiram
Target: Mu-type opioid receptor (GPCR)
Gene: OPRM1
UniProt: P35372 (OPRM_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.846
Assay: DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine)
Drug: disulfiram
Target: Translocator protein (Transporter)
Gene: TSPO
UniProt: P30536 (TSPO_HUMAN)
Organism: Homo sapiens
Drug: disulfiram
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.967
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)