AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: tretinoin
Target: Retinoic acid receptor RXR-beta (Transcription factor)
Gene: Rxrb
UniProt: P28704 (RXRB_MOUSE)
Organism: Mus musculus
Activity: Kd = 6.51
Assay: Inhibition of [3H]9-cis-RA binding to mouse Retinoid X receptor RXR beta
Drug: tretinoin
Target: Retinoic acid receptor RXR-gamma (Transcription factor)
Gene: Rxrg
UniProt: P28705 (RXRG_MOUSE)
Organism: Mus musculus
Activity: Kd = 6.46
Assay: Dissociation constant for binding to Retinoid X receptor gamma
Drug: tretinoin
Target: Cellular retinoic acid-binding protein 1 (Cytosolic other)
Gene: Crabp1
UniProt: P62965 (RABP1_MOUSE)
Organism: Mus musculus
Activity: Kd = 9.4
Assay: Inhibition of [3H]ATRA binding to murine Cytoplasmic retinoic acid binding protein (CRABP) type 1
Drug: tretinoin
Target: Cellular retinoic acid-binding protein 2 (Cytosolic other)
Gene: Crabp2
UniProt: P22935 (RABP2_MOUSE)
Organism: Mus musculus
Activity: Kd = 8.7
Assay: Inhibition of [3H]ATRA binding to murine Cytoplasmic retinoic acid binding protein (CRABP) type 2
Drug: tretinoin
Target: Retinoic acid receptor alpha (Transcription factor)
Gene: Rara
UniProt: P11416 (RARA_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.82
Assay: Dissociation constant for binding to Retinoic acid receptor alpha
Drug: tretinoin
Target: Retinoic acid receptor RXR-alpha (Transcription factor)
Gene: Rxra
UniProt: P28700 (RXRA_MOUSE)
Organism: Mus musculus
Activity: Kd = 6
Assay: Dissociation constant for binding to Retinoid X receptor alpha
Drug: tretinoin
Target: Retinoic acid receptor beta (Transcription factor)
Gene: Rarb
UniProt: P22605 (RARB_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.89
Assay: Dissociation constant for binding to Retinoic acid receptor beta
Drug: tretinoin
Target: Retinoic acid receptor gamma (Transcription factor)
Gene: Rarg
UniProt: P18911 (RARG_MOUSE)
Organism: Mus musculus
Activity: Kd = 7.74
Assay: Dissociation constant for binding to Retinoic acid receptor gamma
Drug: tretinoin
Target: Indoleamine 2,3-dioxygenase 2 (Enzyme)
Gene: Ido2
UniProt: Q8R0V5 (I23O2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.54
Assay: Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Drug: tretinoin
Target: Nuclear receptor subfamily 2 group E member 1 (Nuclear hormone receptor)
Gene: NR2E1
UniProt: Q9Y466 (NR2E1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.74
Action type: AGONIST
Assay: Gal4-DBD TLX LBD screening to determine changes in TLX activity in HEK293 cells.
Drug: tretinoin
Target: Nuclear receptor subfamily 2 group C member 2 (Nuclear other)
Gene: NR2C2
UniProt: P49116 (NR2C2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.62
Action type: AGONIST
Drug: tretinoin
Target: Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Unclassified)
Gene: PIN1
UniProt: Q13526 (PIN1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.09
Assay: Inhibition of human N-terminal His6-tagged Pin1 PPIase activity expressed in Escherichia coli BL21 using Suc-Ala-Glu-cis-Pro-Phe-4-nitroanilide as substrate preincubated for 10 mins followed by substrate addition monitored for 90 secs by protease enzyme coupled based spectrophotometric analysis
Drug: tretinoin
Target: Nuclear receptor subfamily 2 group E member 1 (Nuclear other)
Gene: NR2E1
UniProt: Q9Y466 (NR2E1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.74
Action type: AGONIST
Assay: Gal4-DBD TLX LBD screening to determine changes in TLX activity in HEK293 cells.
Drug: tretoquinol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki  8.27
Drug: tretoquinol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki  7.67
Drug: tretoquinol
Target: Thromboxane A2 receptor (GPCR)
Gene: TBXA2R
UniProt: P21731 (TA2R_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.35
Assay: Inhibitory concentration against radioligand [3H]SQ-29,548 (5 nM) binding to TP receptors in human platelets
Drug: tretoquinol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: Adrb2
UniProt: Q8K4Z4 (ADRB2_CAVPO)
Organism: Cavia porcellus
Activity: EC50 = 7.58
Drug: tretoquinol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: B0FL73 (B0FL73_CAVPO)
Organism: Cavia porcellus
Activity: EC50 = 6.76
Drug: tretoquinol
Target: Adrenergic receptor beta (GPCR)
Gene: ADRB2|ADRB1|ADRB3
UniProt: P07550|P08588|P13945 (ADRB2_HUMAN|ADRB1_HUMAN|ADRB3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.51
Assay: Compound was tested for its intrinsic activity against beta adrenergic receptor of isolated guinea pig atrial pairs
Drug: tretoquinol
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: Ki = 5.3
Assay: Inhibition of [3H]spiroperidol binding to dopamine receptor from rat striatum membranes
Drug: tretoquinol
Target: Adrenergic receptor alpha (GPCR)
Gene: Adra1b|Adra2b|Adra2c|Adra2a|Adra1d|Adra1a
UniProt: P15823|P19328|P22086|P22909|P23944|P43140 (ADA1B_RAT|ADA2B_RAT|ADA2C_RAT|ADA2A_RAT|ADA1D_RAT|ADA1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5
Assay: Inhibition of [3H]WB-4101 binding to alpha adrenergic receptor from rat cerebral cortical membranes
Drug: tretoquinol
Target: Adrenergic receptor beta (GPCR)
Gene: Adrb2|Adrb1|Adrb3
UniProt: P10608|P18090|P26255 (ADRB2_RAT|ADRB1_RAT|ADRB3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7
Assay: Inhibition of [3H]dihydroalprenolol binding to Beta adrenergic receptor from rat cerebral cortical membranes
Drug: triamcinolone
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.585
Action type: AGONIST
Assay: DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone)
Drug: triamcinolone
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: triamcinolone
Target: Progesterone receptor (Nuclear hormone receptor)
Gene: PGR
UniProt: P06401 (PRGR_HUMAN)
Organism: Homo sapiens
Drug: triamcinolone acetonide
Target: Glucocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C1
UniProt: P04150 (GCR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9.3
Action type: AGONIST
Drug: triamcinolone acetonide
Target: Annexin A1 (Cytosolic other)
Gene: ANXA1
UniProt: P04083 (ANXA1_HUMAN)
Organism: Homo sapiens
Drug: triamcinolone acetonide
Target: Progesterone receptor (Transcription factor)
Gene: PGR
UniProt: Q690N0 (Q690N0_BOVIN)
Organism: Bos taurus
Activity: Ki = 7.638
Assay: DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020)
Drug: triamcinolone diacetate
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: triamterene
Target: Solute carrier family 12 member 1 (Transporter)
Gene: SLC12A1
UniProt: Q13621 (S12A1_HUMAN)
Organism: Homo sapiens
Drug: triamterene
Target: Cytochrome P450 2D6 (Enzyme)
Gene: CYP2D6
UniProt: P10635 (CP2D6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: triamterene
Target: Caspase-1 (Enzyme)
Gene: CASP1
UniProt: P29466 (CASP1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.436
Assay: DRUGMATRIX: Protease, Caspase 1 enzyme inhibition (substrate: Ac-YVAD-AMC)
Drug: triamterene
Target: Cathepsin G (Enzyme)
Gene: CTSG
UniProt: P08311 (CATG_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.13
Assay: DRUGMATRIX: Protease, Cathepsin G enzyme inhibition (substrate: Suc-Ala-Ala-Pro-Phe-AMC)
Drug: triamterene
Target: Pteridine reductase 1 (Enzyme)
Gene: PTR1
UniProt: Q01782 (PTR1_LEIMA)
Organism: Leishmania major
Activity: Ki = 5.47
Assay: Inhibition of Leishmania major recombinant PTR1
Drug: triamterene
Target: Amiloride-sensitive sodium channel, ENaC (Ion channel)
Gene: SCNN1A|SCNN1B|SCNN1G
UniProt: P37088|P51168|P51170 (SCNNA_HUMAN|SCNNB_HUMAN|SCNNG_HUMAN)
Organism: Homo sapiens
Activity: IC50 ~ 5.3
Action type: BLOCKER
Assay: Mechanism of Action; CHEMBL2107836; PROTEIN COMPLEX
Drug: triazolam
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.27
Drug: triazolam
Target: Platelet-activating factor receptor (GPCR)
Gene: PTAFR
UniProt: P25105 (PTAFR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.879
Drug: triazolam
Target: Cholecystokinin receptor type A (GPCR)
Gene: Cckar
UniProt: P30551 (CCKAR_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 4.41
Assay: Displacement of [125I]CCK from Cholecystokinin receptor of rat pancreas
Drug: triazolam
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: Ki = 9.155
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA-A receptor alpha-2/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA2
UniProt: P18507|P28472|P47869 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.229
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA-A receptor alpha-3/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA3
UniProt: P18507|P28472|P34903 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.845
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA-A receptor alpha-5/beta-3/gamma-2 (Ion channel)
Gene: GABRG2|GABRB3|GABRA5
UniProt: P18507|P28472|P31644 (GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.02
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA-A receptor alpha-1/beta-2/gamma-3 (Ion channel)
Gene: GABRA1|GABRB2|GABRG3
UniProt: P14867|P47870|Q99928 (GBRA1_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.638
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA-A receptor alpha-1/beta-3/gamma-2 (Ion channel)
Gene: GABRA1|GABRG2|GABRB3
UniProt: P14867|P18507|P28472 (GBRA1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.097
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA-A receptor; anion channel (Ion channel)
Gene: Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre
UniProt: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14 (GBRP_RAT|GBRB1_RAT|GBRD_RAT|GBRG2_RAT|GBRA5_RAT|GBRA3_RAT|GBRG1_RAT|GBRA2_RAT|GBRA4_RAT|GBRG3_RAT|GBRA6_RAT|GBRA1_RAT|GBRB3_RAT|GBRB2_RAT|Q91ZM7_RAT|GBRE_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.1
Assay: Binding affinity for Diazepam sensitive (DS) isoform of the benzodiazepine (Bz) binding site on GABAA receptors
Drug: triazolam
Target: GABA-A receptor (Ion channel)
Gene: GABRD|GABRA1|GABRB1|GABRG2|GABRB3|GABRA5|GABRA3|GABRA2|GABRB2|GABRA4|GABRA6|GABRG1|GABRG3
UniProt: O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|Q16445|Q8N1C3|Q99928 (GBRD_HUMAN|GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN|GBRA3_HUMAN|GBRA2_HUMAN|GBRB2_HUMAN|GBRA4_HUMAN|GBRA6_HUMAN|GBRG1_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.1
Action type: POSITIVE ALLOSTERIC MODULATOR
Assay: Mechanism of Action; CHEMBL2093872; PROTEIN COMPLEX GROUP
Drug: triazolam
Target: GABA A receptor alpha-3/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA3|GABRB2
UniProt: P18507|P34903|P47870 (GBRG2_HUMAN|GBRA3_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.876
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA A receptor alpha-3/beta-2/gamma-3 (Ion channel)
Gene: GABRA3|GABRB2|GABRG3
UniProt: P34903|P47870|Q99928 (GBRA3_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.108
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA A receptor alpha-5/beta-3/gamma-3 (Ion channel)
Gene: GABRB3|GABRA5|GABRG3
UniProt: P28472|P31644|Q99928 (GBRB3_HUMAN|GBRA5_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.699
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA A receptor alpha-5/beta-2/gamma-2 (Ion channel)
Gene: GABRG2|GABRA5|GABRB2
UniProt: P18507|P31644|P47870 (GBRG2_HUMAN|GBRA5_HUMAN|GBRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.222
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: triazolam
Target: GABA A receptor alpha-5/beta-2/gamma-3 (Ion channel)
Gene: GABRA5|GABRB2|GABRG3
UniProt: P31644|P47870|Q99928 (GBRA5_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.699
Action type: POSITIVE ALLOSTERIC MODULATOR
Drug: trichlormethiazide
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.04
Assay: Inhibition of human recombinant full length CA2 by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Solute carrier family 12 member 3 (Transporter)
Gene: SLC12A3
UniProt: P55017 (S12A3_HUMAN)
Organism: Homo sapiens
Activity: A2 = 7
Action type: INHIBITOR
Drug: trichlormethiazide
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.46
Assay: Inhibition of human recombinant full length CA1 by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: P22748 (CAH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.35
Assay: Inhibition of human recombinant full length CA4 by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Carbonic anhydrase 9 (Enzyme)
Gene: CA9
UniProt: Q16790 (CAH9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.06
Assay: Inhibition of human recombinant CA9 catalytic domain by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.51
Assay: Inhibition of human recombinant CA12 catalytic domain by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Carbonic anhydrase 5A, mitochondrial (Enzyme)
Gene: CA5A
UniProt: P35218 (CAH5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.12
Assay: Inhibition of human recombinant full length CA5A by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Carbonic anhydrase 5B, mitochondrial (Enzyme)
Gene: CA5B
UniProt: Q9Y2D0 (CAH5B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.87
Assay: Inhibition of human recombinant full length CA5B by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Carbonic anhydrase 7 (Enzyme)
Gene: CA7
UniProt: P43166 (CAH7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.1
Assay: Inhibition of human recombinant full length CA7 by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Carbonic anhydrase 6 (Enzyme)
Gene: CA6
UniProt: P23280 (CAH6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.61
Assay: Inhibition of human recombinant full length CA6 by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Carbonic anhydrase 14 (Enzyme)
Gene: CA14
UniProt: Q9ULX7 (CAH14_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.46
Assay: Inhibition of human recombinant full length CA14 by stopped-flow CO2 hydration method
Drug: trichlormethiazide
Target: Carbonic anhydrase 13 (Enzyme)
Gene: Ca13
UniProt: Q9D6N1 (CAH13_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.19
Assay: Inhibition of mouse recombinant full length CA13 by stopped-flow CO2 hydration method
Drug: triclabendazole
Target: Cruzipain (Enzyme)
UniProt: P25779 (CYSP_TRYCR)
Organism: Trypanosoma cruzi
Activity: IC50 = 4.82
Assay: Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100
Drug: triclofos
Target: GABA-A receptor; anion channel (Ion channel)
Gene: GABRP|GABRD|GABRA1|GABRB1|GABRG2|GABRB3|GABRA5|GABRA3|GABRA2|GABRB2|GABRA4|GABRE|GABRA6|GABRG1|GABRG3|GABRQ
UniProt: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88 (GBRP_HUMAN|GBRD_HUMAN|GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN|GBRB3_HUMAN|GBRA5_HUMAN|GBRA3_HUMAN|GBRA2_HUMAN|GBRB2_HUMAN|GBRA4_HUMAN|GBRE_HUMAN|GBRA6_HUMAN|GBRG1_HUMAN|GBRG3_HUMAN|GBRT_HUMAN)
Organism: Homo sapiens
Action type: POSITIVE MODULATOR
Assay: Mechanism of Action; CHEMBL2093872; PROTEIN COMPLEX GROUP
Drug: tridihexethyl
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: tridihexethyl
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: trientine
Target: Carbonic anhydrase 2 (Enzyme)
Gene: CA2
UniProt: P00918 (CAH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.19
Assay: Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 1 (Enzyme)
Gene: CA1
UniProt: P00915 (CAH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4
Assay: Inhibition of human carbonic anhydrase 1 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 4 (Enzyme)
Gene: CA4
UniProt: P22748 (CAH4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.46
Assay: Inhibition of human carbonic anhydrase 4 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 9 (Enzyme)
Gene: CA9
UniProt: Q16790 (CAH9_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.41
Assay: Inhibition of human carbonic anhydrase 9 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 12 (Enzyme)
Gene: CA12
UniProt: O43570 (CAH12_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.24
Assay: Inhibition of human carbonic anhydrase 12 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 5A, mitochondrial (Enzyme)
Gene: CA5A
UniProt: P35218 (CAH5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.42
Assay: Inhibition of human carbonic anhydrase 5A by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 5B, mitochondrial (Enzyme)
Gene: CA5B
UniProt: Q9Y2D0 (CAH5B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.31
Assay: Inhibition of human carbonic anhydrase 5B by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 7 (Enzyme)
Gene: CA7
UniProt: P43166 (CAH7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.35
Assay: Inhibition of human carbonic anhydrase 7 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 3 (Enzyme)
Gene: CA3
UniProt: P07451 (CAH3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.32
Assay: Inhibition of human carbonic anhydrase 3 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 6 (Enzyme)
Gene: CA6
UniProt: P23280 (CAH6_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.37
Assay: Inhibition of human carbonic anhydrase 6 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 14 (Enzyme)
Gene: CA14
UniProt: Q9ULX7 (CAH14_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.92
Assay: Inhibition of human carbonic anhydrase 14 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 13 (Enzyme)
Gene: Ca13
UniProt: Q9D6N1 (CAH13_MOUSE)
Organism: Mus musculus
Activity: Ki = 4.28
Assay: Inhibition of mouse carbonic anhydrase 13 by stopped flow CO2 hydration method
Drug: trientine
Target: Carbonic anhydrase 15 (Enzyme)
Gene: Ca15
UniProt: Q99N23 (CAH15_MOUSE)
Organism: Mus musculus
Activity: Ki = 4.23
Assay: Inhibition of mouse carbonic anhydrase 15 by stopped flow CO2 hydration method
Drug: trifluoperazine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.841
Action type: ANTAGONIST
Drug: trifluoperazine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.185
Drug: trifluoperazine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.82
Assay: Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
Drug: trifluoperazine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.292
Assay: DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
Drug: trifluoperazine
Target: 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Enzyme)
Gene: EBP
UniProt: Q15125 (EBP_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.1
Assay: Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand
Drug: trifluoperazine
Target: Multidrug resistance protein 1 (Transporter)
Gene: ABCB1
UniProt: P08183 (MDR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.19
Assay: Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model
Drug: trifluoperazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.022
Drug: trifluoperazine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.9
Action type: ANTAGONIST
Drug: trifluoperazine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.4
Action type: ANTAGONIST
Drug: trifluoperazine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.849
Drug: trifluoperazine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: HTR7
UniProt: P34969 (5HT7R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.536
Drug: trifluoperazine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.62
Drug: trifluoperazine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.786
Drug: trifluoperazine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.251
Action type: ANTAGONIST
Drug: trifluoperazine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.2
Action type: ANTAGONIST
Drug: trifluoperazine
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6
Drug: trifluoperazine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.407
Drug: trifluoperazine
Target: D(4) dopamine receptor (GPCR)
Gene: DRD4
UniProt: P21917 (DRD4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.377
Action type: ANTAGONIST
Drug: trifluoperazine
Target: Calmodulin (Cytosolic other)
Gene: CALM1|CALM2|CALM3
UniProt: P0DP23|P0DP24|P0DP25 (CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6
Assay: Binding affinity to calmodulin
Drug: trifluoperazine
Target: Trypanothione reductase (Enzyme)
Gene: TPR
UniProt: P28593 (TYTR_TRYCR)
Organism: Trypanosoma cruzi
Activity: Ki = 4.64
Assay: Inhibitory activity against recombinant Trypanosoma cruzi (Trypanosoma cruzi) Trypanothione reductase (linear competitive type)
Drug: trifluoperazine
Target: D(2) dopamine receptor (GPCR)
Gene: Drd2
UniProt: P61169 (DRD2_RAT)
Organism: Rattus norvegicus
Activity: Kd = 9.27
Assay: Compound was tested for its effect on dopamine saturation analysis
Drug: trifluoperazine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.39
Assay: Binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 from rat hippocampus