AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: desloratadine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.698
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: nordazepam
Target: Gamma-aminobutyric acid type B receptor subunit 2 (GPCR)
Gene: GABBR2
UniProt: O75899 (GABR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.027
Drug: nordazepam
Target: Gamma-aminobutyric acid receptor subunit rho-2 (Ion channel)
Gene: GABRR2
UniProt: P28476 (GBRR2_HUMAN)
Organism: Homo sapiens
Drug: nordazepam
Target: GABA-A receptor alpha-1/beta-2/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB2
UniProt: P14867|P18507|P47870 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.284
Drug: nordazepam
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabre|Gabra6|Gabrg2|Gabrd|Gabra2|Gabra3|Gabrg3|Gabrb1|Gabra1|Gabrb3|Gabra5|Gabrp|Gabra4|Gabrq|Gabrg1
UniProt: A2AMW3|P16305|P22723|P22933|P26048|P26049|P27681|P50571|P62812|P63080|Q8BHJ7|Q8QZW7|Q9D6F4|Q9JLF1|Q9R0Y8 (A2AMW3_MOUSE|GBRA6_MOUSE|GBRG2_MOUSE|GBRD_MOUSE|GBRA2_MOUSE|GBRA3_MOUSE|GBRG3_MOUSE|GBRB1_MOUSE|GBRA1_MOUSE|GBRB3_MOUSE|GBRA5_MOUSE|GBRP_MOUSE|GBRA4_MOUSE|GBRT_MOUSE|GBRG1_MOUSE)
Organism: Mus musculus
Activity: Ki = 4.14
Assay: Binding affinity for umolar GABA-A central benzodiazepine receptor
Drug: desmopressin
Target: Vasopressin V1a receptor (GPCR)
Gene: AVPR1A
UniProt: P37288 (V1AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.42
Assay: Binding affinity against human vasopressin V1a receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
Drug: desmopressin
Target: Vasopressin V1b receptor (GPCR)
Gene: AVPR1B
UniProt: P47901 (V1BR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.43
Assay: Binding affinity against human vasopressin V1b receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
Drug: desmopressin
Target: Oxytocin receptor (GPCR)
Gene: OXTR
UniProt: P30559 (OXYR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.6
Action type: AGONIST
Drug: desmopressin
Target: Oxytocin receptor (GPCR)
Gene: Oxtr
UniProt: P70536 (OXYR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.01
Assay: Displacement of [3H]AVP from rat OT receptor expressed in CHO cells
Drug: desmopressin
Target: Vasopressin V2 receptor (GPCR)
Gene: Avpr2
UniProt: Q00788 (V2R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.1
Assay: Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug: desmopressin
Target: Vasopressin V1a receptor (GPCR)
Gene: Avpr1a
UniProt: P30560 (V1AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.97
Assay: Displacement of [3H]AVP from vasopressin V1a receptor in rat liver membrane
Drug: desmopressin
Target: Vasopressin V1b receptor (GPCR)
Gene: Avpr1b
UniProt: P48974 (V1BR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.7
Assay: Displacement of [3H]AVP from rat vasopressin V1b receptor expressed in At-T20 cells
Drug: desmopressin
Target: Vasopressin V2 receptor (GPCR)
Gene: AVPR2
UniProt: P30518 (V2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.3
Action type: AGONIST
Assay: Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
Drug: desogestrel
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: desogestrel
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.6
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: desoximetasone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.932
Action type: AGONIST
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: desoximetasone
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: desoximetasone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.959
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: desoxycortone
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki  8.854
Drug: desoxycortone
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.498
Drug: desoxycortone
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki  8.699
Drug: desoxycortone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.2
Action type: AGONIST
Drug: desoxycortone
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 11
Action type: AGONIST
Drug: desoxycortone
Target: Corticosteroid-binding globulin (Secreted)
Gene: SERPINA6
UniProt: P08185 (CBG_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.65
Drug: desoxycortone
Target: Sex hormone-binding globulin (Secreted)
Gene: SHBG
UniProt: P04278 (SHBG_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.38
Assay: Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
Drug: desoxycorticosterone acetate
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL1994; SINGLE PROTEIN
Drug: desoxycorticosterone pivalate
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 11
Action type: AGONIST
Drug: dexamethasone
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.886
Drug: dexamethasone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.88
Action type: AGONIST
Drug: dexamethasone
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: dexamethasone
Target: Interleukin-5 (Cytokine)
Gene: IL5
UniProt: P05113 (IL5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.456
Drug: dexamethasone
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9
Drug: dexamethasone
Target: Interleukin-4 (Cytokine)
Gene: IL4
UniProt: P05112 (IL4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.33
Drug: dexamethasone
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.85
Assay: Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells
Drug: dexamethasone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.25
Assay: Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells
Drug: dexamethasone
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.786
Assay: DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
Drug: dexamethasone
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.66
Assay: Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay
Drug: dexamethasone
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 5.517
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: dexamethasone
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.66
Assay: Displacement of [3H]dexamethasone from Sprague-Dawley rat GR by liquid scintillation counting
Drug: dexamethasone
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: Nr1i2
UniProt: O54915 (NR1I2_MOUSE)
Organism: Mus musculus
Activity: EC50 = 6.1
Action type: AGONIST
Drug: dexamethasone acetate
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
Drug: dexamethasone palmitate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.26
Drug: dexamethasone palmitate
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.48
Drug: dexamethasone palmitate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.85
Drug: dexamethasone palmitate
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.25
Drug: dexamethasone palmitate
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.09
Drug: dexamethasone palmitate
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.66
Drug: dexamethasone palmitate
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.63
Drug: dexamethasone palmitate
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.66
Drug: dexamethasone valerate
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.26
Drug: dexamethasone valerate
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.48
Drug: dexamethasone valerate
Target: Androgen receptor (Nuclear hormone receptor)
Gene: AR
UniProt: P10275 (ANDR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.85
Drug: dexamethasone valerate
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.25
Drug: dexamethasone valerate
Target: Androgen receptor (Transcription factor)
Gene: Ar
UniProt: P15207 (ANDR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.09
Drug: dexamethasone valerate
Target: Fatty acid-binding protein, liver (Unclassified)
Gene: Fabp1
UniProt: P02692 (FABPL_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.66
Drug: dexamethasone valerate
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: IC50 = 4.63
Drug: dexamethasone valerate
Target: Glucocorticoid receptor (Transcription factor)
Gene: Nr3c1
UniProt: P06536 (GCR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.66
Drug: dexbrompheniramine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Drug: dexetimide
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.9
Action type: ANTAGONIST
Drug: dexetimide
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.8
Action type: ANTAGONIST
Drug: dexetimide
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: Chrm1|Chrm4|Chrm5|Chrm3|Chrm2
UniProt: P12657|P32211|Q920H4|Q9ERZ3|Q9ERZ4 (ACM1_MOUSE|ACM4_MOUSE|ACM5_MOUSE|ACM3_MOUSE|ACM2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.48
Assay: Ability (10 ug/kg) to inhibit binding of [125I]iododexetimide to muscarinic receptor in mice
Drug: dexfenfluramine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.002
Drug: dexfenfluramine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.275
Drug: dexfenfluramine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.664
Assay: DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
Drug: dexfenfluramine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.176
Drug: dexfenfluramine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.08
Drug: dexfenfluramine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.607
Drug: dexfenfluramine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.384
Drug: dexfenfluramine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.79
Drug: dexfenfluramine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.042
Drug: dexfenfluramine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.257
Drug: dexfenfluramine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.57
Drug: dexfenfluramine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.62
Drug: dexfenfluramine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.733
Drug: dexfenfluramine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.577
Drug: dexfenfluramine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.326
Drug: dexfenfluramine
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.156
Drug: dexfenfluramine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.72
Drug: dexfenfluramine
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.898
Drug: dexfenfluramine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.706
Drug: dexfenfluramine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.848
Drug: dexfenfluramine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 5.47
Drug: dexketoprofen
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.57
Action type: INHIBITOR
Assay: Concentration required for 50% inhibition against Prostaglandin G/H synthase 2 from human
Drug: dexketoprofen
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.72
Action type: INHIBITOR
Assay: Concentration required for 50% inhibition against Prostaglandin G/H synthase 1 from human
Drug: dexloxiglumide
Target: Cholecystokinin receptor type A (GPCR)
Gene: CCKAR
UniProt: P32238 (CCKAR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.886
Drug: dexmedetomidine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.82
Action type: AGONIST
Assay: Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
Drug: dexmedetomidine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.7
Drug: dexmedetomidine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.7
Action type: AGONIST
Drug: dexmedetomidine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.3
Action type: AGONIST
Drug: dexmedetomidine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10.82
Assay: In vitro binding affinity against alpha-2D adrenergic receptor of male Wistar rat
Drug: dexmedetomidine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.5
Drug: dexmedetomidine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: Adra2a
UniProt: P22909 (ADA2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 10.82
Assay: Binding affinity towards alpha-2D adrenergic receptor
Drug: dexmedetomidine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: EC50 = 6.42
Assay: Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug: dexmedetomidine
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 = 10.82
Assay: In vitro binding affinity against alpha-2 adrenergic receptor in rat
Drug: dexmedetomidine
Target: Adrenergic receptor alpha-1 (GPCR)
Gene: Adra1b|Adra1d|Adra1a
UniProt: P15823|P23944|P43140 (ADA1B_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.3
Assay: Tested for Binding affinity towards alpha-1 adrenergic receptor
Drug: dexmedetomidine
Target: Alpha-1B adrenergic receptor (GPCR)
UniProt: G3HDX1 (G3HDX1_CRIGR)
Organism: Cricetulus griseus
Activity: EC50 = 6.44
Assay: Agonist activity at hamster recombinant alpha-1B receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
Drug: dexmethylphenidate
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: dexmethylphenidate
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: SLC6A3
UniProt: Q01959 (SC6A3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.8
Action type: INHIBITOR
Assay: Displacement of [3H]WIN-35,428 from human DAT expressed in mouse N2A cells after 15 mins by liquid scintillation counting
Drug: dexmethylphenidate
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.13
Assay: Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat striatum
Drug: dexmethylphenidate
Target: Transporter (Transporter)
Gene: Slc6a2
UniProt: Q9WTR4 (Q9WTR4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.57
Assay: Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat cortical tissue
Drug: dexmethylphenidate
Target: Dopamine receptor (GPCR)
Gene: Drd1|Drd3|Drd5|Drd4|Drd2
UniProt: P18901|P19020|P25115|P30729|P61169 (DRD1_RAT|DRD3_RAT|DRD5_RAT|DRD4_RAT|DRD2_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.08
Assay: Potency of inhibiting [3H]WIN-35428 binding to dopamine receptor in rat striatal membranes
Drug: dexniguldipine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.05
Assay: Ability to displace [3H]rauwolscine from cloned human Alpha-2A adrenergic receptor
Drug: dexniguldipine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.432
Drug: dexniguldipine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 10
Assay: GRAC: human a1A selective antagonist
Drug: dexniguldipine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.18
Assay: Ability to displace [3H]rauwolscine from cloned human Alpha-2B adrenergic receptor
Drug: dexniguldipine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.35
Assay: Ability to displace [3H]rauwolscine from cloned human Alpha-2C adrenergic receptor
Drug: dexniguldipine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.72
Assay: Displacement of [125 I]AB-MECA from human Adenosine A3 receptor expressed in HEK cells
Drug: dexniguldipine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.77
Assay: Ability to displace [3H]prazosin from cloned human Alpha-1D adrenergic receptor
Drug: dexniguldipine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.25
Assay: Ability to displace [3H]prazosin from cloned human Alpha-1B adrenergic receptor
Drug: dexniguldipine
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.824
Drug: dexniguldipine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.42
Assay: Binding affinity towards Alpha-1B adrenergic receptor in rat liver using [3H]prazosin as radioligand
Drug: dexniguldipine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.2
Assay: Binding affinity towards Alpha-1A adrenergic receptor in rat hippocampal membranes using [3H]prazosin as radioligand
Drug: dexniguldipine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: Adra1d
UniProt: P23944 (ADA1D_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.08
Assay: Binding affinity towards Alpha-1D adrenergic receptor in rat brain using [3H]prazosin as radioligand
Drug: dexniguldipine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.53
Assay: Binding affinity towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand
Drug: dexniguldipine
Target: Adenosine receptor A1 (GPCR)
Gene: Adora1
UniProt: P25099 (AA1R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.38
Assay: Displacement of [3H]R-PIA from Adenosine A1 receptor of rat brain membrane
Drug: dexniguldipine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P18130 (ADA1A_BOVIN)
Organism: Bos taurus
Activity: Ki = 9.42
Assay: Binding affinity towards Alpha-1A adrenergic receptor in bovine brain using [3H]prazosin as radioligand