AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: niclosamide
Target: Mast/stem cell growth factor receptor Kit (Kinase)
Gene: KIT
UniProt: P10721 (KIT_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.56
Assay: Inhibition of KIT after 60 mins by radiometric assay
Drug: niclosamide
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.98
Assay: Inhibition of EGFR after 60 mins by radiometric assay
Drug: niclosamide
Target: Proto-oncogene tyrosine-protein kinase Src (Kinase)
Gene: SRC
UniProt: P12931 (SRC_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: Inhibition of Src kinase
Drug: niclosamide
Target: Vascular endothelial growth factor receptor 2 (Kinase)
Gene: KDR
UniProt: P35968 (VGFR2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.64
Assay: Inhibition of VEGFR2 after 60 mins by radiometric assay
Drug: niclosamide
Target: Tyrosine-protein kinase JAK2 (Kinase)
Gene: JAK2
UniProt: O60674 (JAK2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5
Assay: Inhibition of JAK2
Drug: niclosamide
Target: Angiopoietin-1 receptor (Kinase)
Gene: TEK
UniProt: Q02763 (TIE2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.17
Assay: Inhibition of TIE2 after 60 mins by radiometric assay
Drug: niclosamide
Target: Tyrosine-protein kinase Lyn (Kinase)
Gene: LYN
UniProt: P07948 (LYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.62
Assay: Inhibition of LYN after 60 mins by radiometric assay
Drug: niclosamide
Target: Fibroblast growth factor receptor 1 (Kinase)
Gene: FGFR1
UniProt: P11362 (FGFR1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.88
Assay: Inhibition of FGFR-1 after 60 mins by radiometric assay
Drug: niclosamide
Target: Aurora kinase A (Kinase)
Gene: AURKA
UniProt: O14965 (AURKA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.27
Assay: Inhibition of Aurora-A after 60 mins by radiometric assay
Drug: niclosamide
Target: RAC-alpha serine/threonine-protein kinase (Kinase)
Gene: AKT1
UniProt: P31749 (AKT1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.23
Assay: Inhibition of Akt1 after 60 mins by radiometric assay
Drug: niclosamide
Target: Glycogen synthase kinase-3 beta (Kinase)
Gene: GSK3B
UniProt: P49841 (GSK3B_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.11
Assay: Inhibition of GSK3-beta after 60 mins by radiometric assay
Drug: niclosamide
Target: 3-phosphoinositide-dependent protein kinase 1 (Kinase)
Gene: PDPK1
UniProt: O15530 (PDPK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.08
Assay: Inhibition of PDK1 after 60 mins by radiometric assay
Drug: niclosamide
Target: Potassium channel subfamily T member 1 (Ion channel)
Gene: KCNT1
UniProt: Q5JUK3 (KCNT1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 5.54
Action type: ACTIVATOR
Drug: niclosamide
Target: Signal transducer and activator of transcription 3 (Transcription factor)
Gene: STAT3
UniProt: P40763 (STAT3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.6
Assay: Inhibition of STAT3 in human HeLa cells after 24 hrs by luciferase reporter gene assay
Drug: niclosamide
Target: Replicase polyprotein 1ab (Enzyme)
Gene: rep
UniProt: P0C6X7 (R1AB_CVHSA)
Organism: Human SARS coronavirus
Activity: IC50 = 4.4
Assay: Inhibition of SARS Co-V 3CL protease
Drug: nicorandil
Target: ATP-sensitive inward rectifier potassium channel 11 (Ion channel)
Gene: KCNJ11
UniProt: Q14654 (KCJ11_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.886
Drug: nicorandil
Target: ATP-sensitive inward rectifier potassium channel 1 (Ion channel)
Gene: KCNJ1
UniProt: P48048 (KCNJ1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.95
Drug: nicorandil
Target: Atrial natriuretic peptide receptor 1 (Enzyme)
Gene: NPR1
UniProt: P16066 (ANPRA_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.2
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: CHRNA7
UniProt: P36544 (ACHA7_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.39
Drug: nicotine
Target: Potassium voltage-gated channel subfamily D member 3 (Ion channel)
Gene: KCND3
UniProt: Q9UK17 (KCND3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.4
Drug: nicotine
Target: Cytochrome P450 2A6 (Enzyme)
Gene: CYP2A6
UniProt: P11509 (CP2A6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.356
Drug: nicotine
Target: Acetylcholine-binding protein (Unclassified)
UniProt: P58154 (ACHP_LYMST)
Organism: Lymnaea stagnalis
Activity: Ki = 7.2
Assay: Displacement of [125I]alpha-bungarotoxin from Lymnaea stagnalis His-tagged AchBP
Drug: nicotine
Target: Transient receptor potential cation channel subfamily A member 1 (Ion channel)
Gene: TRPA1
UniProt: O75762 (TRPA1_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 4.8
Action type: ACTIVATOR
Assay: Patch clamp
Drug: nicotine
Target: Acetylcholine receptor subunit delta (Ion channel)
Gene: chrnd
UniProt: P02718 (ACHD_TORCA)
Organism: Torpedo californica
Activity: Ki = 9
Assay: Bindind affinity values obtained by measuring the displacement of radioligand [3H](-)-cytisine from a preparation of whole rat brain
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-4 (Ion channel)
Gene: Chrna4
UniProt: P09483 (ACHA4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9.03
Assay: Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: Chrna7
UniProt: Q05941 (ACHA7_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.89
Assay: Binding affinity to subtype Nicotinic acetylcholine receptor alpha-7 using [125I]-alpha-BTX as radioligand in rat brain
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-7 (Ion channel)
Gene: Chrna7
UniProt: P49582 (ACHA7_MOUSE)
Organism: Mus musculus
Activity: Ki = 6.61
Assay: Displacement of [125I]-alpha-Btx from alpha7 nAChR in mouse hippocampal membranes
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-9 (Ion channel)
Gene: Chrna9
UniProt: P43144 (ACHA9_RAT)
Organism: Rattus norvegicus
Activity: Kd = 8.3
Assay: The compound was tested for the inhibition of binding of [3H]epibatidine to central nicotinic acetylcholine receptor (nAChR) in rat brain.
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit beta-4 (Ion channel)
Gene: Chrnb4
UniProt: P12392 (ACHB4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.14
Assay: Binding affinity to Nicotinic acetylcholine receptor alpha3-beta4 using +/-[3H]epibatidine as radioligand in pig adrenal gland
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-3 (Ion channel)
Gene: Chrna3
UniProt: P04757 (ACHA3_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.33
Assay: Displacement of [3H]epibatidine from rat alpha3beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-2 (Ion channel)
Gene: Chrna2
UniProt: P12389 (ACHA2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.92
Assay: Displacement of [3H]epibatidine from rat alpha2beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting
Drug: nicotine
Target: Soluble acetylcholine receptor (Unclassified)
UniProt: Q8WSF8 (Q8WSF8_APLCA)
Organism: Aplysia californica
Activity: Ki = 7.52
Assay: Binding affinity to salt water mollusc Aplysia californica AChBP Y55W mutant assessed as [3H]acetamiprid binding by radioligand binding assay
Drug: nicotine
Target: Acetylcholine receptor subunit alpha (Ion channel)
Gene: CHRNA1
UniProt: P02710 (ACHA_TORCA)
Organism: Torpedo californica
Activity: IC50 = 4.64
Assay: Displacement of [3H]alpha-BGT from nAChR in Torpedo nobiliana electric organs
Drug: nicotine
Target: Lycopene cyclase (Enzyme)
Gene: crtY
UniProt: P21687 (CRTY_PANAN)
Organism: Pantoea ananas
Activity: IC50 = 5.32
Assay: Inhibition of Pantoea ananatis lycopene cyclase
Drug: nicotine
Target: Nicotinic acetylcholine receptor alpha 5 subunit (Ion channel)
Gene: nAChRalpha5
UniProt: A9XFY4 (A9XFY4_MUSDO)
Organism: Musca domestica
Activity: Ki = 5.61
Assay: Displacement of [3H]alpha-bungarotoxin from nAChR in Musca domestica (house fly) head membrane after 60 min by scintillation counting
Drug: nicotine
Target: Acetylcholine receptor subunit beta-like 2 (Ion channel)
Gene: nAChRbeta2
UniProt: P25162 (ACH4_DROME)
Organism: Drosophila melanogaster
Activity: Ki = 5.57
Assay: Binding affinity to Drosophila brain nicotinic acetylcholine receptor assessed as [3H]IMI binding by radioligand binding assay
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-4 (Ion channel)
Gene: CHRNA4
UniProt: P09482 (ACHA4_CHICK)
Organism: Gallus gallus
Activity: Ki = 8.72
Assay: Binding affinity to recombinant Gallus gallus (chicken) alpha4beta2 nicotinic acetylcholine receptor assessed as [3H]NIC binding by radioligand binding assay
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-4 (Ion channel)
Gene: Chrna4
UniProt: O70174 (ACHA4_MOUSE)
Organism: Mus musculus
Activity: IC50 = 8.15
Assay: Inhibition of [3H]nicotine binding to alpha4 nicotinic acetylcholine receptor in Mus musculus (mouse) M10 cells co-expressing beta2 nicotinic acetylcholine receptor subunits
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha2/beta2 (Ion channel)
Gene: Chrna2|Chrnb2
UniProt: P12389|P12390 (ACHA2_RAT|ACHB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.26
Assay: Displacement of [3H]epibatidine from rat nAChR alpha2beta2
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha3/beta2 (Ion channel)
Gene: Chrna3|Chrnb2
UniProt: P04757|P12390 (ACHA3_RAT|ACHB2_RAT)
Organism: Rattus norvegicus
Activity: Ki = 9
Assay: Affinity for Nicotinic acetylcholine receptor alpha4-beta2 tested by analogue-induced inhibition of [3H]NIC binding to rat striatal membranes
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha3/beta4 (Ion channel)
Gene: Chrna3|Chrnb4
UniProt: P04757|P12392 (ACHA3_RAT|ACHB4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 6.7
Assay: Displacement of [3H]epibatidine from recombinant rat alpha-3-beta-4 nAChr in HEK293 cell line
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: Chrna4|Chrnb2
UniProt: P09483|P12390 (ACHA4_RAT|ACHB2_RAT)
Organism: Rattus norvegicus
Activity: Kd = 9.4
Assay: GRAC: rat AChR-alpha4-beta2 radioligand
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha4/beta4 (Ion channel)
Gene: Chrna4|Chrnb4
UniProt: P09483|P12392 (ACHA4_RAT|ACHB4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.26
Assay: Displacement of [3H]epibatidine from rat alpha2beta2 nACHR
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha2/beta4 (Ion channel)
Gene: CHRNB4|CHRNA2
UniProt: P30926|Q15822 (ACHB4_HUMAN|ACHA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.15
Assay: Displacement of [3H]epibatidine from alpha2beta4 nAChR after 4 hrs by liquid scintillation counting analysis
Drug: nicotine
Target: Neuronal acetylcholine receptor (Ion channel)
Gene: Chrna3|Chrna4|Chrna2|Chrnb2|Chrnb3|Chrnb4|Chrna5|Chrna1|Chrnb1|Chrna6|Chrna9|Chrna7|Chrna10
UniProt: P04757|P09483|P12389|P12390|P12391|P12392|P20420|P25108|P25109|P43143|P43144|Q05941|Q9JLB5 (ACHA3_RAT|ACHA4_RAT|ACHA2_RAT|ACHB2_RAT|ACHB3_RAT|ACHB4_RAT|ACHA5_RAT|ACHA_RAT|ACHB_RAT|ACHA6_RAT|ACHA9_RAT|ACHA7_RAT|ACH10_RAT)
Organism: Rattus norvegicus
Activity: Kd = 11
Assay: Ability to enhance the binding of (+/-)-[3H]nicotine to the rat brain P2 fraction at binding site 2
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha2/beta2 (Ion channel)
Gene: CHRNB2|CHRNA2
UniProt: P17787|Q15822 (ACHB2_HUMAN|ACHA2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.26
Assay: Displacement of [3H]epibatidine from alpha2beta2 nAChR after 4 hrs by liquid scintillation counting analysis
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha4/beta2 (Ion channel)
Gene: CHRNB2|CHRNA4
UniProt: P17787|P43681 (ACHB2_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.56
Action type: AGONIST
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha3/beta4 (Ion channel)
Gene: CHRNB4|CHRNA3
UniProt: P30926|P32297 (ACHB4_HUMAN|ACHA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.95
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha3/beta2 (Ion channel)
Gene: CHRNB2|CHRNA3
UniProt: P17787|P32297 (ACHB2_HUMAN|ACHA3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.854
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha4/beta4 (Ion channel)
Gene: CHRNB4|CHRNA4
UniProt: P30926|P43681 (ACHB4_HUMAN|ACHA4_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.64
Assay: Displacement of [3H]epibatidine from alpha4beta4 nAChR after 4 hrs by liquid scintillation counting analysis
Drug: nicotine
Target: Serotonin 3 (5-HT3) receptor (Ion channel)
Gene: HTR3E|HTR3B|HTR3A|HTR3D|HTR3C
UniProt: A5X5Y0|O95264|P46098|Q70Z44|Q8WXA8 (5HT3E_HUMAN|5HT3B_HUMAN|5HT3A_HUMAN|5HT3D_HUMAN|5HT3C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.15
Assay: In vitro Binding affinity towards 5-hydroxytryptamine 3 receptor was determined
Drug: nicotine
Target: Acetylcholine receptor; alpha1/beta1/delta/gamma (Ion channel)
Gene: CHRNA1|CHRNG|CHRNB1|CHRND
UniProt: P02708|P07510|P11230|Q07001 (ACHA_HUMAN|ACHG_HUMAN|ACHB_HUMAN|ACHD_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.83
Assay: Binding affinity to alpha-1-beta-gamma-delta nicotinic receptor
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha3/alpha6/beta2/beta3 (Ion channel)
Gene: CHRNB2|CHRNA3|CHRNB3|CHRNA6
UniProt: P17787|P32297|Q05901|Q15825 (ACHB2_HUMAN|ACHA3_HUMAN|ACHB3_HUMAN|ACHA6_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.07
Assay: Antagonist activity at human alpha6/alpha3beta2beta3 nAChR expressed in human SHEP1 cells assessed as inhibition of carbamylcholine-induced 86Rb+ ion efflux preincubated for 10 mins by liquid scintillation counting analysis
Drug: nicotine
Target: Neuronal acetylcholine receptor; alpha2/beta4 (Ion channel)
Gene: Chrna2|Chrnb4
UniProt: P12389|P12392 (ACHA2_RAT|ACHB4_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.15
Assay: Displacement of [3H]epibatidine from rat nAChR alpha2beta4
Drug: nicotine
Target: Acetylcholine receptor (Ion channel)
Gene: CHRNA1|CHRNB1|CHRNG|chrnd
UniProt: P02710|P02712|P02714|P02718 (ACHA_TORCA|ACHB_TORCA|ACHG_TORCA|ACHD_TORCA)
Organism: Torpedo californica
Activity: Ki = 5.2
Assay: Inhibition of [125I]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha1 beta gamma delta of electroplax
Drug: nicotine
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: IC50 = 4.55
Assay: Inhibitory concentration required for in vitro binding affinity to cholinergic central muscarinic receptor on rat brain cortex by using [3H]OXO-M
Drug: nicotine
Target: Acetylcholine receptor subunit alpha (Ion channel)
Gene: CHRNA1
UniProt: P02708 (ACHA_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.68
Assay: Inhibition of [3H]alpha-BGT binding to alpha1 nicotinic acetylcholine receptor in Homo sapiens (human) TE671 cells co-expressing gammaalpha1deltabeta1 nicotinic acetylcholine receptor subunits
Drug: nicotine
Target: Neuronal acetylcholine receptor subunit alpha-3 (Ion channel)
Gene: CHRNA3
UniProt: P32297 (ACHA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.35
Assay: Inhibition of [3H]nicotine binding to alpha3 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells co-expressing beta2beta4alpha5 Nicotinic acetylcholine receptor subunits
Drug: nicotine
Target: Transient receptor potential cation channel subfamily A member 1 (Ion channel)
Gene: Trpa1
UniProt: Q8BLA8 (TRPA1_MOUSE)
Organism: Mus musculus
Activity: EC50 = 5
Assay: Agonist activity at mouse TRPA1 expressed in CHO cells assessed as increase in calcium influx by patch clamp electrophysiology method
Drug: nicotine
Target: Potassium voltage-gated channel subfamily D member 3 (Ion channel)
Gene: Kcnd3
UniProt: Q62897 (KCND3_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.4
Action type: BLOCKER
Drug: nifedipine
Target: Sodium/nucleoside cotransporter 1 (Transporter)
Gene: SLC28A1
UniProt: O00337 (S28A1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.089
Assay: DRUGMATRIX: Sodium/nucleoside co-transporter radioligand binding (ligand: nitrobenzylthioinosine)
Drug: nifedipine
Target: Adenosine receptor A2a (GPCR)
Gene: ADORA2A
UniProt: P29274 (AA2AR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.65
Assay: Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells
Drug: nifedipine
Target: Potassium voltage-gated channel subfamily H member 2 (Ion channel)
Gene: KCNH2
UniProt: Q12809 (KCNH2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.3
Drug: nifedipine
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.26
Drug: nifedipine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.495
Drug: nifedipine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.019
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: nifedipine
Target: Adenosine receptor A1 (GPCR)
Gene: ADORA1
UniProt: P30542 (AA1R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.348
Assay: DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)
Drug: nifedipine
Target: Adenosine receptor A3 (GPCR)
Gene: ADORA3
UniProt: P0DMS8 (AA3R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.08
Assay: Inhibition of [125I]- AB-MECA binding to human Adenosine A3 receptors expressed in HEK cells
Drug: nifedipine
Target: Glutathione reductase, mitochondrial (Enzyme)
Gene: GSR
UniProt: P00390 (GSHR_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.76
Assay: Competitive inhibition of human erythrocyte Glutathione reductase using GSSG substrate by Lineweaver-Burk plot analysis
Drug: nifedipine
Target: Transthyretin (Secreted)
Gene: TTR
UniProt: P02766 (TTHY_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.658
Drug: nifedipine
Target: Glycine receptor subunit alpha-1 (Ion channel)
Gene: GLRA1
UniProt: P23415 (GLRA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.48
Assay: GRAC: human Glycine receptor subunit alpha-1 selective antagonist
Drug: nifedipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: CACNA1D
UniProt: Q01668 (CAC1D_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.7
Action type: GATING INHIBITOR
Assay: Recombinant Cav1.3 calcium channel complexes expressed in tsA-cells
Drug: nifedipine
Target: Bile salt export pump (Transporter)
Gene: ABCB11
UniProt: O95342 (ABCBB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.51
Drug: nifedipine
Target: Voltage-dependent T-type calcium channel subunit alpha-1H (Ion channel)
Gene: CACNA1H
UniProt: O95180 (CAC1H_HUMAN)
Organism: Homo sapiens
Activity: Ki = 4.672
Drug: nifedipine
Target: Cytochrome P450 1A2 (Enzyme)
Gene: CYP1A2
UniProt: P05177 (CP1A2_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.523
Assay: DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
Drug: nifedipine
Target: Potassium voltage-gated channel subfamily A member 1 (Ion channel)
Gene: KCNA1
UniProt: Q09470 (KCNA1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.02
Assay: Inhibition of Kv1.1 (unknown origin)
Drug: nifedipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1S (Ion channel)
Gene: CACNA1S
UniProt: Q13698 (CAC1S_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6.3
Action type: INHIBITOR
Drug: nifedipine
Target: Potassium voltage-gated channel subfamily A member 5 (Ion channel)
Gene: KCNA5
UniProt: P22460 (KCNA5_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.21
Assay: Inhibition of human Kv1.5 channel expressed in mouse L929 cells by EP voltage clamp technique
Drug: nifedipine
Target: cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Enzyme)
Gene: PDE4A
UniProt: P27815 (PDE4A_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.355
Assay: DRUGMATRIX: Phosphodiesterase PDE4 enzyme inhibition (substrate: [3H]cAMP + cAMP)
Drug: nifedipine
Target: Glycine receptor subunit beta (Ion channel)
Gene: GLRB
UniProt: P48167 (GLRB_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.9
Action type: ANTAGONIST
Drug: nifedipine
Target: Potassium voltage-gated channel subfamily A member 2 (Ion channel)
Gene: KCNA2
UniProt: P16389 (KCNA2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 4.7
Drug: nifedipine
Target: Myosin light chain kinase, smooth muscle (Kinase)
Gene: MYLK
UniProt: Q15746 (MYLK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.69
Drug: nifedipine
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.731
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: nifedipine
Target: C-C chemokine receptor type 2 (GPCR)
Gene: CCR2
UniProt: P41597 (CCR2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.072
Assay: DRUGMATRIX: Chemokine CCR2B  radioligand binding (ligand: [125I] MCP-1)
Drug: nifedipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1F (Ion channel)
Gene: CACNA1F
UniProt: O60840 (CAC1F_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Action type: GATING INHIBITOR
Drug: nifedipine
Target: Glycine receptor subunit alpha-3 (Ion channel)
Gene: GLRA3
UniProt: O75311 (GLRA3_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.5
Action type: ANTAGONIST
Drug: nifedipine
Target: Arachidonate 15-lipoxygenase (Enzyme)
Gene: ALOX15
UniProt: P12530 (LOX15_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 4.821
Assay: DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid)
Drug: nifedipine
Target: Adenosine receptor A1 (GPCR)
Gene: Adora1
UniProt: P25099 (AA1R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 5.54
Assay: Binding affinity against adenosine A1 receptor in rat cerebral cortex membrane by radioligand binding assay using [3H](R)-PIA.
Drug: nifedipine
Target: Acetylcholinesterase (Enzyme)
Gene: ache
UniProt: O42275 (ACES_ELEEL)
Organism: Electrophorus electricus
Activity: Ki = 5.4
Assay: Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) assessed as inhibition of ATCh hydrolysis by Ellman method
Drug: nifedipine
Target: Adenosine receptor A2a (GPCR)
Gene: Adora2a
UniProt: P30543 (AA2AR_RAT)
Organism: Rattus norvegicus
Activity: Ki = 4.74
Assay: Displacement of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal membranes
Drug: nifedipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: CACNA1C
UniProt: P15381 (CAC1C_RABIT)
Organism: Oryctolagus cuniculus
Activity: IC50 = 9
Assay: Inhibition of [3H]nitrendipine binding to calcium channels in Rabbit cardiac muscle.
Drug: nifedipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1C (Ion channel)
Gene: Cacna1c
UniProt: P22002 (CAC1C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.46
Assay: Inhibition of [3H](+)-PN200-110 binding to L-type calcium channel 1,4-DHP binding site of rat ventricular myocytes
Drug: nifedipine
Target: Voltage-dependent L-type calcium channel subunit alpha-1D (Ion channel)
Gene: Cacna1d
UniProt: P27732 (CAC1D_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.92
Assay: Binding affinity for L-type [Ca2+] channels was measured through displacement of [3H]nitrendipine on rat cortex homogenates.
Drug: nifedipine
Target: Cholinesterase (Enzyme)
Gene: BCHE
UniProt: P81908 (CHLE_HORSE)
Organism: Equus caballus
Activity: Ki = 5.92
Assay: Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method
Drug: nifedipine
Target: Indoleamine 2,3-dioxygenase 2 (Enzyme)
Gene: Ido2
UniProt: Q8R0V5 (I23O2_MOUSE)
Organism: Mus musculus
Activity: IC50 = 5.82
Assay: Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis