AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: candesartan cilexetil
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.51
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: candesartan cilexetil
Target: Type-1 angiotensin II receptor (GPCR)
Gene: AGTR1
UniProt: P25104 (AGTR1_BOVIN)
Organism: Bos taurus
Activity: IC50 = 6.96
Drug: candesartan cilexetil
Target: Cruzipain (Enzyme)
UniProt: P25779 (CYSP_TRYCR)
Organism: Trypanosoma cruzi
Activity: IC50 = 4.38
Assay: Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100
Drug: candesartan cilexetil
Target: Type-1 angiotensin II receptor (GPCR)
Gene: AGTR1
UniProt: P34976 (AGTR1_RABIT)
Organism: Oryctolagus cuniculus
Activity: Ki = 9.19
Drug: candesartan cilexetil
Target: DNULL polymerase kappa (Enzyme)
Gene: POLK
UniProt: Q9UBT6 (POLK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.25
Assay: Inhibition of human DNA polymerase kappa (19 to 526 residues)-mediated TLS past acrolein derived ring-opened reduced form of gamma-HOPdG lesions preincubated for 15 mins followed by DNA substrate addition measured after 30 mins in presence of dCTP and dGTP by radioactive gel-based primer extension assay
Drug: candesartan cilexetil
Target: DNULL polymerase iota (Enzyme)
Gene: POLI
UniProt: Q9UNA4 (POLI_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.21
Assay: Inhibition of human DNA polymerase iota preincubated for 15 mins followed by replicating non-damaged DNA substrate addition measured after 30 mins in presence of dCTP and dGTP by radioactive gel-based primer extension assay
Drug: candesartan cilexetil
Target: DNULL polymerase eta (Enzyme)
Gene: POLH
UniProt: Q9Y253 (POLH_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.95
Assay: Inhibition of human DNA polymerase eta (1 to 437 residues) preincubated for 15 mins followed by replicating non-damaged DNA substrate addition measured after 30 mins in presence of dCTP and dGTP by radioactive gel-based primer extension assay
Drug: candesartan cilexetil
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.05
Assay: DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
Drug: candesartan cilexetil
Target: Sodium-dependent noradrenaline transporter (Transporter)
Gene: SLC6A2
UniProt: P23975 (SC6A2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.52
Assay: DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)
Drug: candesartan cilexetil
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.76
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: candesartan cilexetil
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.49
Assay: DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: candesartan cilexetil
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.16
Assay: DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)
Drug: candesartan cilexetil
Target: Cytochrome P450 2C9 (Enzyme)
Gene: CYP2C9
UniProt: P11712 (CP2C9_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.52
Assay: DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: candesartan cilexetil
Target: Type-1 angiotensin II receptor (GPCR)
Gene: AGTR1
UniProt: P30556 (AGTR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.16
Action type: ANTAGONIST
Assay: Displacement of [3H]-Angiotensin 2 from human AT1 receptor transfected in CHOK1 cells preincubated for 30 mins with bovine serum albumin followed by radioligand addition by liquid scintillation counting
Drug: candesartan cilexetil
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.48
Assay: DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: candesartan cilexetil
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.23
Assay: DRUGMATRIX: Protein Tyrosine Kinase, ERBB2 (HER2) enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: canrenone
Target: Mineralocorticoid receptor (Nuclear hormone receptor)
Gene: NR3C2
UniProt: P08235 (MCR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.523
Action type: ANTAGONIST
Assay: inhibitION the aldosterone-induced MR activity
Drug: capecitabine
Target: Thymidylate synthase (Enzyme)
Gene: TYMS
UniProt: P04818 (TYSY_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: captopril
Target: Prostaglandin G/H synthase 2 (Enzyme)
Gene: PTGS2
UniProt: P35354 (PGH2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.92
Assay: Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method
Drug: captopril
Target: Prostaglandin G/H synthase 1 (Enzyme)
Gene: PTGS1
UniProt: P23219 (PGH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.77
Assay: Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method
Drug: captopril
Target: Angiotensin-converting enzyme (Enzyme)
Gene: ACE
UniProt: P12821 (ACE_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Action type: INHIBITOR
Drug: captopril
Target: Prothrombin (Enzyme)
Gene: F2
UniProt: P00734 (THRB_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.32
Assay: Inhibitory activity against thrombin
Drug: captopril
Target: Renin (Enzyme)
Gene: REN
UniProt: P00797 (RENI_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.77
Assay: Antihypertensive activity against human renin
Drug: captopril
Target: Leukotriene A-4 hydrolase (Enzyme)
Gene: LTA4H
UniProt: P09960 (LKHA4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.15
Assay: Inhibitory activity against Leukotriene A4 hydrolase from human leukocytes
Drug: captopril
Target: Angiotensin-converting enzyme (Enzyme)
Gene: ACE
UniProt: P12822 (ACE_RABIT)
Organism: Oryctolagus cuniculus
Activity: Ki = 8.77
Assay: Inhibitory activity against rabbit lung angiotensin-1 converting enzyme
Drug: captopril
Target: Angiotensin-converting enzyme (Enzyme)
Gene: Ace
UniProt: P47820 (ACE_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.7
Assay: Inhibition of Angiotensin I converting enzyme (ACE)
Drug: captopril
Target: Succinyl-diaminopimelate desuccinylase (Enzyme)
Gene: dapE
UniProt: P44514 (DAPE_HAEIN)
Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Activity: Ki = 5.74
Assay: Inhibition of Haemophilus influenzae recombinant DapE by competitive binding assay
Drug: captopril
Target: Beta-lactamase (Enzyme)
Gene: blaIMP-1
UniProt: Q79MP6 (Q79MP6_PSEAI)
Organism: Pseudomonas aeruginosa
Activity: Ki = 5.62
Assay: Inhibition of recombinant Pseudomonas aeruginosa MBL IMP-1 using nitrocefin as substrate preincubated for 20 mins by UV-spectrophotometric analysis
Drug: captopril
Target: Beta-lactamase II (Enzyme)
Gene: bla2
UniProt: Q93T40 (Q93T40_BACAN)
Organism: Bacillus anthracis
Activity: Ki = 4.75
Assay: Inhibition of Bacillus anthracis MBL Bla2 using nitrocefin as substrate preincubated for 20 mins by UV-spectrophotometric analysis
Drug: captopril
Target: Beta-lactamase class B VIM-2 (Unclassified)
Gene: blaVIM-2
UniProt: Q9K2N0 (Q9K2N0_PSEAI)
Organism: Pseudomonas aeruginosa
Activity: Kd = 6.22
Drug: captopril
Target: Beta-lactamase NDM-1 (Enzyme)
Gene: blaNDM-1
UniProt: C7C422 (BLAN1_KLEPN)
Organism: Klebsiella pneumoniae
Activity: Kd = 4.85
Assay: Binding affinity to His-tagged Klebsiella pneumoniae NDM-1 expressed in Escherichia coli BL21-AI cells by surface plasmon resonance assay
Drug: caramiphen
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.81
Assay: Binding affinity against Sigma receptor type 1 was determined by the displacement of [3H]pentazocine radioligand
Drug: caramiphen
Target: Lysosomal Pro-X carboxypeptidase (Enzyme)
Gene: PRCP
UniProt: P42785 (PCP_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.59
Assay: Inhibition of [3H]- (+) - pentazocine binding to PCP receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum
Drug: caramiphen
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.5
Assay: Displacement of [3H](-)-quinuclidinyl benzilate(QNB) from muscarinic (M2) receptor in rat heart homogenates
Drug: caramiphen
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.92
Assay: Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 in rat cortex homogenates
Drug: caramiphen
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.29
Assay: Binding affinity against dopamine transporter was determined by the displacement of [3H]WIN-35428 radioligand in rat brain
Drug: carazolol
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.94
Assay: Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter
Drug: carazolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: ADRB3
UniProt: P13945 (ADRB3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Action type: AGONIST
Drug: carazolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: Adrb3
UniProt: P25962 (ADRB3_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.7
Action type: AGONIST
Drug: carazolol
Target: Beta-3 adrenergic receptor (GPCR)
Gene: Adrb3
UniProt: P26255 (ADRB3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.7
Action type: AGONIST
Drug: carazolol
Target: Beta-1 adrenergic receptor (GPCR)
Gene: Adrb1
UniProt: P34971 (ADRB1_MOUSE)
Organism: Mus musculus
Activity: Ki = 10.05
Assay: Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
Drug: carbachol
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.523
Drug: carbachol
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.921
Drug: carbachol
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.699
Action type: AGONIST
Drug: carbachol
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: CHRM4
UniProt: P08173 (ACM4_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.577
Drug: carbachol
Target: Muscarinic acetylcholine receptor M5 (GPCR)
Gene: CHRM5
UniProt: P08912 (ACM5_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.097
Drug: carbachol
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: CHRNA7
UniProt: P36544 (ACHA7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.18
Assay: Binding affinity to alpha7 nAChR (unknown origin)
Drug: carbachol
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: P10980 (ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.4
Assay: Binding affinity at [3H]CD radiolabeled muscarinic M2 receptor in rat cortex.
Drug: carbachol
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P08482 (ACM1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.51
Assay: Affinity versus [3H]oxotremorine M (agonist) binding to Muscarinic acetylcholine receptor M1 in Rat Cerebral Cortical Membranes, (Kd=0.75 nM)
Drug: carbachol
Target: Acetylcholine receptor subunit delta (Ion channel)
Gene: chrnd
UniProt: P02718 (ACHD_TORCA)
Organism: Torpedo californica
Activity: Ki = 6.35
Assay: Binding affinity towards rat forebrain nicotinic acetylcholine receptor using [3H]EB as radioligand
Drug: carbachol
Target: Acetylcholinesterase (Enzyme)
Gene: Ache
UniProt: P21836 (ACES_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.1
Assay: Compound was evaluated for the binding affinity by displacing [3H]oxotremorine from mouse cerebral cortex tissue.
Drug: carbachol
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: Chrm1
UniProt: P12657 (ACM1_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.7
Assay: Binding affinity (low) of [3H](R)-QNB binding to Muscarinic acetylcholine receptor M1 expressed in A9 L cell line in the absence of 300 uM GTP-gamma-S
Drug: carbachol
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: Chrm2
UniProt: Q9ERZ4 (ACM2_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.1
Assay: Ability to displace [3H]oxotremorine ([3H]OXO-M) from mouse cerebral cortex
Drug: carbachol
Target: Muscarinic acetylcholine receptor M4 (GPCR)
Gene: Chrm4
UniProt: P08485 (ACM4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.59
Assay: Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
Drug: carbachol
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: GPM3
UniProt: Q8VH26 (Q8VH26_CAVPO)
Organism: Cavia porcellus
Activity: Kd = 4.74
Assay: Dissociation constant for complex with muscarinic acetylcholine receptor M3 of guinea pig ileum
Drug: carbachol
Target: Acetylcholine receptor subunit alpha (Ion channel)
Gene: CHRNA1
UniProt: P02710 (ACHA_TORCA)
Organism: Torpedo californica
Activity: IC50 = 5.12
Assay: Displacement of [3H]alpha-BGT from nAChR in Torpedo nobiliana electric organs
Drug: carbachol
Target: Neuronal acetylcholine receptor; alpha2/beta2 (Ion channel)
Gene: Chrna2|Chrnb2
UniProt: P12389|P12390 (ACHA2_RAT|ACHB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.68
Assay: Binding affinity towards rat nicotinic acetylcholine receptor alpha2-beta2 expressed in HEK293 cells using [3H]EB as radioligand
Drug: carbachol
Target: Neuronal acetylcholine receptor; alpha3/beta2 (Ion channel)
Gene: Chrna3|Chrnb2
UniProt: P04757|P12390 (ACHA3_RAT|ACHB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.96
Assay: Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand
Drug: carbachol
Target: Neuronal acetylcholine receptor; alpha3/beta4 (Ion channel)
Gene: Chrna3|Chrnb4
UniProt: P04757|P12392 (ACHA3_RAT|ACHB4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.32
Assay: Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in HEK293 cells using [3H]EB as radioligand
Drug: carbachol
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: Chrna4|Chrnb2
UniProt: P09483|P12390 (ACHA4_RAT|ACHB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.23
Assay: Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in HEK293 cells using [3H]EB as radioligand
Drug: carbachol
Target: Neuronal acetylcholine receptor; alpha4/beta4 (Ion channel)
Gene: Chrna4|Chrnb4
UniProt: P09483|P12392 (ACHA4_RAT|ACHB4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.89
Assay: Binding affinity towards rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in HEK293 cells using [3H]EB as radioligand
Drug: carbachol
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: CHRNB2|CHRNA4
UniProt: P17787|P43681 (ACHB2_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.12
Assay: Binding affinity to alpha4beta2 nAChR (unknown origin)
Drug: carbachol
Target: Muscarinic acetylcholine receptor (GPCR)
Gene: Chrm1|Chrm3|Chrm4|Chrm5|Chrm2
UniProt: P08482|P08483|P08485|P08911|P10980 (ACM1_RAT|ACM3_RAT|ACM4_RAT|ACM5_RAT|ACM2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.89
Assay: In vitro binding affinity for muscarinic receptor by displacing [3H]oxotremorine-M binding on rat brain homogenate.
Drug: carbamazepine
Target: Sodium channel protein type 5 subunit alpha (Ion channel)
Gene: SCN5A
UniProt: Q14524 (SCN5A_HUMAN)
Organism: Homo sapiens
Action type: BLOCKER
Drug: carbamazepine
Target: Sodium-dependent serotonin transporter (Transporter)
Gene: SLC6A4
UniProt: P31645 (SC6A4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.495
Drug: carbamazepine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.125
Drug: carbamazepine
Target: Sodium channel protein type 4 subunit alpha (Ion channel)
Gene: SCN4A
UniProt: P35499 (SCN4A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.28
Action type: BLOCKER
Assay: Affinity for inactive human SkM1 sodium channel expressed in HEK293 cells
Drug: carbamazepine
Target: Sodium channel protein type 9 subunit alpha (Ion channel)
Gene: SCN9A
UniProt: Q15858 (SCN9A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.66
Action type: BLOCKER
Assay: Blockade of human Nav1.7 channel expressed in HEK293 cells by FRET assay
Drug: carbamazepine
Target: Nuclear receptor subfamily 1 group I member 2 (Nuclear hormone receptor)
Gene: NR1I2
UniProt: O75469 (NR1I2_HUMAN)
Organism: Homo sapiens
Drug: carbamazepine
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
Drug: carbamazepine
Target: Neuronal acetylcholine receptor; alpha2/beta4 (Ion channel)
Gene: CHRNB4|CHRNA2
UniProt: P30926|Q15822 (ACHB4_HUMAN|ACHA2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.31
Drug: carbamazepine
Target: Frizzled-8 (GPCR)
Gene: FZD8
UniProt: Q9H461 (FZD8_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.77
Action type: ALLOSTERIC MODULATOR
Assay: Binding affinity for FZD8 cysteine-rich domain (CRD) by SPR analysis.
Drug: carbenicillin
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.37
Drug: carbenicillin
Target: Muscarinic acetylcholine receptor M3 (GPCR)
Gene: CHRM3
UniProt: P20309 (ACM3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Drug: carbenicillin
Target: Penicillin-binding protein 1A (Enzyme)
Gene: pbpA
UniProt: Q8XJ01 (PBPA_CLOPE)
Organism: Clostridium perfringens (strain 13 / Type A)
Drug: carbenicillin
Target: Bacterial penicillin-binding protein (Enzyme)
Gene: mrcA|mrcB|dacC|mrdA|ftsI|dacA|dacB
UniProt: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228 (PBPA_ECOLI|PBPB_ECOLI|DACC_ECOLI|PBP2_ECOLI|FTSI_ECOLI|DACA_ECOLI|DACB_ECOLI)
Organism: Escherichia coli (strain K12)
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL2354204; PROTEIN FAMILY
Drug: carbenoxolone
Target: Corticosteroid 11-beta-dehydrogenase isozyme 1 (Enzyme)
Gene: HSD11B1
UniProt: P28845 (DHI1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.08
Action type: INHIBITOR
Assay: Ability to convert [3H]cortisol to the tritium labeled cortisone in the presence of human 11 beta hydroxysteroid dehydrogenase type 2
Drug: carbenoxolone
Target: Corticosteroid 11-beta-dehydrogenase isozyme 1 (Enzyme)
Gene: Hsd11b1
UniProt: P50172 (DHI1_MOUSE)
Organism: Mus musculus
Activity: IC50 = 6.97
Assay: In vitro inhibitory activity against mouse 11 beta hydroxysteroid dehydrogenase type 1 using scintillation proximity assay (SPA).
Drug: carbenoxolone
Target: Corticosteroid 11-beta-dehydrogenase isozyme 2 (Enzyme)
Gene: Hsd11b2
UniProt: P51661 (DHI2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 7.09
Assay: Inhibition of mouse microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
Drug: pentoxyverine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: SIGMAR1
UniProt: Q99720 (SGMR1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.71
Assay: Binding affinity against Sigma receptor type 1 was determined by the displacement of [3H]pentazocine radioligand
Drug: pentoxyverine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.12
Assay: Binding affinity towards muscarinic m1 receptor
Drug: pentoxyverine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.78
Assay: Binding affinity towards muscarinic m2 receptor
Drug: pentoxyverine
Target: Lysosomal Pro-X carboxypeptidase (Enzyme)
Gene: PRCP
UniProt: P42785 (PCP_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.49
Assay: Inhibition of [3H]- (+) - pentazocine binding to PCP receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum
Drug: pentoxyverine
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.81
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Drug: pentoxyverine
Target: Sodium-dependent dopamine transporter (Transporter)
Gene: Slc6a3
UniProt: P23977 (SC6A3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.51
Assay: Binding affinity against dopamine transporter was determined by the displacement of [3H]WIN-35428 radioligand in rat brain
Drug: pentoxyverine
Target: Sigma non-opioid intracellular receptor 1 (Membrane receptor)
Gene: Sigmar1
UniProt: Q9R0C9 (SGMR1_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.96
Assay: Tested for its binding affinity towards sigma-1 site in presence of [3H]- -(+)3 PPP
Drug: carbetocin
Target: Vasopressin V1a receptor (GPCR)
Gene: AVPR1A
UniProt: P37288 (V1AR_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.39
Drug: carbetocin
Target: Vasopressin V2 receptor (GPCR)
Gene: AVPR2
UniProt: P30518 (V2R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.232
Assay: vasopressin V2 receptors expressed in COS-7 cells
Drug: carbetocin
Target: Oxytocin receptor (GPCR)
Gene: OXTR
UniProt: P30559 (OXYR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.149
Action type: AGONIST
Assay: oxytocin receptors expressed in COS-7 cells
Drug: carbidopa
Target: Aromatic-L-amino-acid decarboxylase (Enzyme)
Gene: DDC
UniProt: P20711 (DDC_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Assay: Mechanism of Action; CHEMBL1843; SINGLE PROTEIN
Drug: carbidopa
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.168
Assay: DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: carbidopa
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.428
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: carbidopa
Target: Lysine-specific demethylase 4E (Enzyme)
Gene: KDM4E
UniProt: B2RXH2 (KDM4E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.7
Assay: Uncompetitive inhibition of JMJD2E relative to alpha-ketoglutarate
Drug: carbimazole
Target: Lactoperoxidase (Enzyme)
Gene: LPO
UniProt: P22079 (PERL_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.98
Assay: Inhibition of lactoperoxidase-catalyzed iodination of L-tyrosine assessed as 3,5-diiodo-L-tyrosine formation by HPLC
Drug: carbimazole
Target: Thyroid peroxidase (Enzyme)
Gene: TPO
UniProt: P07202 (PERT_HUMAN)
Organism: Homo sapiens
Action type: INHIBITOR
Drug: carbinoxamine
Target: Histamine H1 receptor (GPCR)
Gene: HRH1
UniProt: P35367 (HRH1_HUMAN)
Organism: Homo sapiens
Action type: ANTAGONIST
Assay: Mechanism of Action; CHEMBL231; SINGLE PROTEIN
Drug: carboprost
Target: Prostaglandin F2-alpha receptor (GPCR)
Gene: PTGFR
UniProt: P43088 (PF2R_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Assay: Mechanism of Action; CHEMBL1987; SINGLE PROTEIN
Drug: carbutamide
Target: Sulfonylurea receptor 1, Kir6.2 (Ion channel)
Gene: ABCC8|KCNJ11
UniProt: Q09428|Q14654 (ABCC8_HUMAN|KCJ11_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.602
Action type: BLOCKER
Assay: [86]Rb+ efflux in RINm5F insulinoma cells