AIM-Harvard/TrialPanorama-filtered huggingface dataset:
Drug: ergometrine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.53
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: ergometrine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8
Drug: ergometrine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.201
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.333
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 8.5
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.58
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.959
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.824
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide)
Drug: ergometrine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.879
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: ergometrine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.714
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 9
Drug: ergometrine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: ADRA1B
UniProt: P35368 (ADA1B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.367
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: EC50 = 7.7
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.889
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.09
Drug: ergometrine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.5
Action type: AGONIST
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 4 (GPCR)
Gene: HTR4
UniProt: O70528 (5HT4R_CAVPO)
Organism: Cavia porcellus
Activity: Ki = 6.578
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT4 radioligand binding (ligand: [3H] GR-113808)
Drug: ergotamine
Target: Beta-1 adrenergic receptor (GPCR)
Gene: ADRB1
UniProt: P08588 (ADRB1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.621
Assay: DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)
Drug: ergotamine
Target: Beta-2 adrenergic receptor (GPCR)
Gene: ADRB2
UniProt: P07550 (ADRB2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 5.722
Assay: DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)
Drug: ergotamine
Target: D(1A) dopamine receptor (GPCR)
Gene: DRD1
UniProt: P21728 (DRD1_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.063
Assay: DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug: ergotamine
Target: D(2) dopamine receptor (GPCR)
Gene: DRD2
UniProt: P14416 (DRD2_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.845
Assay: DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone)
Drug: ergotamine
Target: Alpha-2A adrenergic receptor (GPCR)
Gene: ADRA2A
UniProt: P08913 (ADA2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.099
Assay: DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
Drug: ergotamine
Target: Cytochrome P450 3A4 (Enzyme)
Gene: CYP3A4
UniProt: P08684 (CP3A4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 6
Assay: DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin)
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: HTR1A
UniProt: P08908 (5HT1A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.354
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: HTR2A
UniProt: P28223 (5HT2A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9
Action type: AGONIST
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 2B (GPCR)
Gene: HTR2B
UniProt: P41595 (5HT2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.9
Action type: AGONIST
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: HTR2C
UniProt: P28335 (5HT2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.7
Action type: AGONIST
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: HTR6
UniProt: P50406 (5HT6R_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.6
Action type: AGONIST
Drug: ergotamine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: ADRA1A
UniProt: P35348 (ADA1A_HUMAN)
Organism: Homo sapiens
Action type: AGONIST
Drug: ergotamine
Target: Alpha-2B adrenergic receptor (GPCR)
Gene: ADRA2B
UniProt: P18089 (ADA2B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.754
Assay: DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)
Drug: ergotamine
Target: D(3) dopamine receptor (GPCR)
Gene: DRD3
UniProt: P35462 (DRD3_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.836
Assay: DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
Drug: ergotamine
Target: D(1B) dopamine receptor (GPCR)
Gene: DRD5
UniProt: P21918 (DRD5_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.77
Drug: ergotamine
Target: Muscarinic acetylcholine receptor M1 (GPCR)
Gene: CHRM1
UniProt: P11229 (ACM1_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.064
Drug: ergotamine
Target: Muscarinic acetylcholine receptor M2 (GPCR)
Gene: CHRM2
UniProt: P08172 (ACM2_HUMAN)
Organism: Homo sapiens
Activity: Ki  6.04
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: HTR1B
UniProt: P28222 (5HT1B_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.68
Assay: Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 1D (GPCR)
Gene: HTR1D
UniProt: P28221 (5HT1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 9.1
Action type: AGONIST
Assay: Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 1D receptor
Drug: ergotamine
Target: Alpha-2C adrenergic receptor (GPCR)
Gene: ADRA2C
UniProt: P18825 (ADA2C_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.742
Assay: DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)
Drug: ergotamine
Target: Alpha-1D adrenergic receptor (GPCR)
Gene: ADRA1D
UniProt: P25100 (ADA1D_HUMAN)
Organism: Homo sapiens
Activity: Ki = 8.487
Assay: DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: HTR5A
UniProt: P47898 (5HT5A_HUMAN)
Organism: Homo sapiens
Activity: Ki = 7.85
Assay: Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: HTR1F
UniProt: P30939 (5HT1F_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.8
Action type: AGONIST
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 1E (GPCR)
Gene: HTR1E
UniProt: P28566 (5HT1E_HUMAN)
Organism: Homo sapiens
Activity: Ki = 6.3
Action type: AGONIST
Drug: ergotamine
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.187
Assay: DRUGMATRIX: Protein Tyrosine Kinase, LCK enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: ergotamine
Target: Tyrosine-protein kinase Fyn (Kinase)
Gene: FYN
UniProt: P06241 (FYN_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.5
Assay: DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr))
Drug: ergotamine
Target: Thromboxane-A synthase (Enzyme)
Gene: TBXAS1
UniProt: P24557 (THAS_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.514
Assay: DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
Drug: ergotamine
Target: Alpha-1B adrenergic receptor (GPCR)
Gene: Adra1b
UniProt: P15823 (ADA1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.342
Assay: DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 1B (GPCR)
Gene: Htr1b
UniProt: P28564 (5HT1B_RAT)
Organism: Rattus norvegicus
Activity: Ki = 10.041
Assay: DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug: ergotamine
Target: Alpha-1A adrenergic receptor (GPCR)
Gene: Adra1a
UniProt: P43140 (ADA1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 8.09
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 1A (GPCR)
Gene: Htr1a
UniProt: P19327 (5HT1A_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 9.11
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 2A (GPCR)
Gene: Htr2a
UniProt: P14842 (5HT2A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8
Action type: AGONIST
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 7 (GPCR)
Gene: Htr7
UniProt: P32304 (5HT7R_MOUSE)
Organism: Mus musculus
Activity: Ki = 7.3
Action type: ANTAGONIST
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 2C (GPCR)
Gene: Htr2c
UniProt: P08909 (5HT2C_RAT)
Organism: Rattus norvegicus
Activity: Ki = 7.9
Action type: AGONIST
Drug: ergotamine
Target: Gastrin/cholecystokinin type B receptor (GPCR)
Gene: Cckbr
UniProt: P56481 (GASR_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.77
Assay: Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKB in mouse fore brain membranes
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 6 (GPCR)
Gene: Htr6
UniProt: P31388 (5HT6R_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.6
Action type: AGONIST
Drug: ergotamine
Target: Cholecystokinin A receptor (GPCR)
Gene: Cckar
UniProt: O08786 (CCKAR_MOUSE)
Organism: Mus musculus
Activity: IC50 = 4.47
Assay: Concentration of compound required to inhibit binding of [125I]J-BH-CCK-8 radioligand to CCKA in mouse pancreatic membranes
Drug: ergotamine
Target: Adenylate cyclase (Unclassified)
Gene: cyaC
UniProt: O32393 (O32393_ARTPT)
Organism: Arthrospira platensis
Activity: IC50 = 4.15
Assay: Inhibition of Spirulina platensis adenylyl cyclase assessed as cAMP level by cAMP immunogenic assay
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: Htr5a
UniProt: P35364 (5HT5A_RAT)
Organism: Rattus norvegicus
Activity: Ki = 8.2
Action type: ANTAGONIST
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 5A (GPCR)
Gene: Htr5a
UniProt: P30966 (5HT5A_MOUSE)
Organism: Mus musculus
Activity: Ki = 8.4
Action type: ANTAGONIST
Drug: ergotamine
Target: 5-hydroxytryptamine receptor 1F (GPCR)
Gene: Htr1f
UniProt: P30940 (5HT1F_RAT)
Organism: Rattus norvegicus
Activity: IC50 = 7.3
Action type: AGONIST
Drug: eritoran
Target: Toll-like receptor 4 (Membrane receptor)
Gene: TLR4
UniProt: O00206 (TLR4_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 8.82
Assay: Antagonist activity at TLR4 in human serum assessed as reduction in LPS-induced TNFalpha production after 3 hrs by ELISA
Drug: erlotinib
Target: Tyrosine-protein kinase JAK3 (Kinase)
Gene: JAK3
UniProt: P52333 (JAK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.15
Assay: Binding constant for JAK3(JH1domain-catalytic) kinase domain
Drug: erlotinib
Target: Platelet-derived growth factor receptor beta (Kinase)
Gene: PDGFRB
UniProt: P09619 (PGFRB_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.85
Assay: Binding constant for PDGFRB kinase domain
Drug: erlotinib
Target: Tyrosine-protein kinase ABL1 (Kinase)
Gene: ABL1
UniProt: P00519 (ABL1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.24
Assay: Binding constant for ABL1(H396P)-phosphorylated kinase domain
Drug: erlotinib
Target: Mast/stem cell growth factor receptor Kit (Kinase)
Gene: KIT
UniProt: P10721 (KIT_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.89
Assay: Binding constant for KIT(V559D,T670I) kinase domain
Drug: erlotinib
Target: Epidermal growth factor receptor (Kinase)
Gene: EGFR
UniProt: P00533 (EGFR_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 9.22
Action type: INHIBITOR
Drug: erlotinib
Target: Proto-oncogene tyrosine-protein kinase Src (Kinase)
Gene: SRC
UniProt: P12931 (SRC_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.15
Assay: Binding constant for SRC kinase domain
Drug: erlotinib
Target: Tyrosine-protein kinase Lck (Kinase)
Gene: LCK
UniProt: P06239 (LCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.6
Assay: Binding constant for LCK kinase domain
Drug: erlotinib
Target: Tyrosine-protein kinase Yes (Kinase)
Gene: YES1
UniProt: P07947 (YES_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.66
Assay: Binding constant for YES kinase domain
Drug: erlotinib
Target: Serine/threonine-protein kinase B-raf (Kinase)
Gene: BRAF
UniProt: P15056 (BRAF_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 7.22
Assay: Inhibition of recombinant full-length GST-tagged human B-RAF V600E mutant (417 to 766 residues) expressed in Baculovirus infected Sf9 cells using N-terminal His-tagged human MEK1 as substrate by Nu-page gel-based phosphor screen analysis
Drug: erlotinib
Target: Receptor-type tyrosine-protein kinase FLT3 (Kinase)
Gene: FLT3
UniProt: P36888 (FLT3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.89
Assay: Binding constant for FLT3(D835Y) kinase domain
Drug: erlotinib
Target: Proto-oncogene tyrosine-protein kinase receptor Ret (Kinase)
Gene: RET
UniProt: P07949 (RET_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.48
Assay: Binding constant for RET(M918T) kinase domain
Drug: erlotinib
Target: Vascular endothelial growth factor receptor 1 (Kinase)
Gene: FLT1
UniProt: P17948 (VGFR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.36
Assay: Binding constant for FLT1 kinase domain
Drug: erlotinib
Target: Vascular endothelial growth factor receptor 2 (Kinase)
Gene: KDR
UniProt: P35968 (VGFR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.24
Assay: Binding constant for VEGFR2 kinase domain
Drug: erlotinib
Target: Vascular endothelial growth factor receptor 3 (Kinase)
Gene: FLT4
UniProt: P35916 (VGFR3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.68
Assay: Binding constant for FLT4 kinase domain
Drug: erlotinib
Target: Platelet-derived growth factor receptor alpha (Kinase)
Gene: PDGFRA
UniProt: P16234 (PGFRA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.74
Assay: Binding constant for PDGFRA kinase domain
Drug: erlotinib
Target: Receptor tyrosine-protein kinase erbB-2 (Kinase)
Gene: ERBB2
UniProt: P04626 (ERBB2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.54
Assay: Binding constant for ERBB2 kinase domain
Drug: erlotinib
Target: Death-associated protein kinase 3 (Kinase)
Gene: DAPK3
UniProt: O43293 (DAPK3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.22
Assay: Binding constant for DAPK3 kinase domain
Drug: erlotinib
Target: Focal adhesion kinase 1 (Kinase)
Gene: PTK2
UniProt: Q05397 (FAK1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 5.13
Assay: Inhibition of FAK (unknown origin) assembly preincubated with enzyme followed by GTP addition measured after 20 mins by spectrophotometric analysis
Drug: erlotinib
Target: Tyrosine-protein kinase HCK (Kinase)
Gene: HCK
UniProt: P08631 (HCK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.74
Assay: Binding constant for HCK kinase domain
Drug: erlotinib
Target: Receptor tyrosine-protein kinase erbB-4 (Kinase)
Gene: ERBB4
UniProt: Q15303 (ERBB4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.64
Assay: Binding constant for ERBB4 kinase domain
Drug: erlotinib
Target: Mitogen-activated protein kinase 10 (Kinase)
Gene: MAPK10
UniProt: P53779 (MK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.37
Assay: Binding constant for JNK3 kinase domain
Drug: erlotinib
Target: Tyrosine-protein kinase JAK2 (Kinase)
Gene: JAK2
UniProt: O60674 (JAK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.43
Assay: Binding constant for JAK2(JH1domain-catalytic) kinase domain
Drug: erlotinib
Target: Calcium/calmodulin-dependent protein kinase type II subunit delta (Kinase)
Gene: CAMK2D
UniProt: Q13557 (KCC2D_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.19
Assay: Binding constant for CAMK2D kinase domain
Drug: erlotinib
Target: Myosin light chain kinase 2, skeletal/cardiac muscle (Kinase)
Gene: MYLK2
UniProt: Q9H1R3 (MYLK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.01
Assay: Binding constant for MYLK2 kinase domain
Drug: erlotinib
Target: Tyrosine-protein kinase CSK (Kinase)
Gene: CSK
UniProt: P41240 (CSK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.02
Assay: Binding constant for CSK kinase domain
Drug: erlotinib
Target: Ephrin type-A receptor 8 (Kinase)
Gene: EPHA8
UniProt: P29322 (EPHA8_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.03
Assay: Binding constant for EPHA8 kinase domain
Drug: erlotinib
Target: AP2-associated protein kinase 1 (Kinase)
Gene: AAK1
UniProt: Q2M2I8 (AAK1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.92
Assay: Binding constant for AAK1 kinase domain
Drug: erlotinib
Target: Hepatocyte growth factor receptor (Kinase)
Gene: MET
UniProt: P08581 (MET_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for MET(Y1235D) kinase domain
Drug: erlotinib
Target: Tyrosine-protein kinase Lyn (Kinase)
Gene: LYN
UniProt: P07948 (LYN_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.28
Assay: Binding constant for LYN kinase domain
Drug: erlotinib
Target: Serine/threonine-protein kinase 17B (Kinase)
Gene: STK17B
UniProt: O94768 (ST17B_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.03
Assay: Binding constant for DRAK2 kinase domain
Drug: erlotinib
Target: Serine/threonine-protein kinase 10 (Kinase)
Gene: STK10
UniProt: O94804 (STK10_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.72
Assay: Binding constant for LOK kinase domain
Drug: erlotinib
Target: Serine/threonine-protein kinase PLK4 (Kinase)
Gene: PLK4
UniProt: O00444 (PLK4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.72
Assay: Binding constant for PLK4 kinase domain
Drug: erlotinib
Target: Aurora kinase C (Kinase)
Gene: AURKC
UniProt: Q9UQB9 (AURKC_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.22
Assay: Binding constant for full-length AURKC
Drug: erlotinib
Target: Dual specificity protein kinase TTK (Kinase)
Gene: TTK
UniProt: P33981 (TTK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.43
Assay: Binding constant for TTK kinase domain
Drug: erlotinib
Target: Abelson tyrosine-protein kinase 2 (Kinase)
Gene: ABL2
UniProt: P42684 (ABL2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.7
Assay: Binding constant for ABL2 kinase domain
Drug: erlotinib
Target: Ephrin type-A receptor 5 (Kinase)
Gene: EPHA5
UniProt: P54756 (EPHA5_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.15
Assay: Binding constant for EPHA5 kinase domain
Drug: erlotinib
Target: Fibroblast growth factor receptor 2 (Kinase)
Gene: FGFR2
UniProt: P21802 (FGFR2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.72
Assay: Average Binding Constant for FGFR2; NA=Not Active at 10 uM
Drug: erlotinib
Target: Serine/threonine-protein kinase 17A (Kinase)
Gene: STK17A
UniProt: Q9UEE5 (ST17A_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.2
Assay: Binding constant for DRAK1 kinase domain
Drug: erlotinib
Target: Ephrin type-A receptor 6 (Kinase)
Gene: EPHA6
UniProt: Q9UF33 (EPHA6_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.36
Assay: Binding constant for EPHA6 kinase domain
Drug: erlotinib
Target: TRAF2 and NCK-interacting protein kinase (Kinase)
Gene: TNIK
UniProt: Q9UKE5 (TNIK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.35
Assay: Binding constant for TNIK kinase domain
Drug: erlotinib
Target: Casein kinase I isoform epsilon (Kinase)
Gene: CSNK1E
UniProt: P49674 (KC1E_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.3
Assay: Binding constant for CSNK1E kinase domain
Drug: erlotinib
Target: Tyrosine-protein kinase Fgr (Kinase)
Gene: FGR
UniProt: P09769 (FGR_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for FGR kinase domain
Drug: erlotinib
Target: Aurora kinase A (Kinase)
Gene: AURKA
UniProt: O14965 (AURKA_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.66
Assay: Binding constant for AURKA kinase domain
Drug: erlotinib
Target: ALK tyrosine kinase receptor (Kinase)
Gene: ALK
UniProt: Q9UM73 (ALK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.92
Assay: Binding constant for ALK kinase domain
Drug: erlotinib
Target: Serine/threonine-protein kinase 36 (Kinase)
Gene: STK36
UniProt: Q9NRP7 (STK36_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.36
Assay: Binding constant for STK36 kinase domain
Drug: erlotinib
Target: Ephrin type-A receptor 3 (Kinase)
Gene: EPHA3
UniProt: P29320 (EPHA3_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.62
Assay: Binding constant for EPHA3 kinase domain
Drug: erlotinib
Target: BMP-2-inducible protein kinase (Kinase)
Gene: BMP2K
UniProt: Q9NSY1 (BMP2K_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.92
Assay: Binding constant for BIKE kinase domain
Drug: erlotinib
Target: Tyrosine-protein kinase FRK (Kinase)
Gene: FRK
UniProt: P42685 (FRK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.7
Assay: Binding constant for FRK kinase domain
Drug: erlotinib
Target: Cyclin-G-associated kinase (Kinase)
Gene: GAK
UniProt: O14976 (GAK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 8.51
Assay: Binding constant for GAK kinase domain
Drug: erlotinib
Target: Receptor-interacting serine/threonine-protein kinase 2 (Kinase)
Gene: RIPK2
UniProt: O43353 (RIPK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.39
Assay: Average Binding Constant for RIPK2; NA=Not Active at 10 uM
Drug: erlotinib
Target: Ephrin type-B receptor 1 (Kinase)
Gene: EPHB1
UniProt: P54762 (EPHB1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.96
Assay: Binding constant for EPHB1 kinase domain
Drug: erlotinib
Target: Ephrin type-A receptor 7 (Kinase)
Gene: EPHA7
UniProt: Q15375 (EPHA7_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.85
Assay: Binding constant for EPHA7 kinase domain
Drug: erlotinib
Target: STE20-like serine/threonine-protein kinase (Kinase)
Gene: SLK
UniProt: Q9H2G2 (SLK_HUMAN)
Organism: Homo sapiens
Activity: Kd = 7.59
Assay: Binding constant for SLK kinase domain
Drug: erlotinib
Target: MAP kinase-interacting serine/threonine-protein kinase 2 (Kinase)
Gene: MKNK2
UniProt: Q9HBH9 (MKNK2_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6
Assay: Binding constant for MKNK2 kinase domain
Drug: erlotinib
Target: Mitogen-activated protein kinase 9 (Kinase)
Gene: MAPK9
UniProt: P45984 (MK09_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.7
Assay: Binding constant for JNK2 kinase domain
Drug: erlotinib
Target: Epithelial discoidin domain-containing receptor 1 (Kinase)
Gene: DDR1
UniProt: Q08345 (DDR1_HUMAN)
Organism: Homo sapiens
Activity: Kd = 6.1
Assay: Binding constant for DDR1 kinase domain
Drug: erlotinib
Target: Solute carrier family 22 member 1 (Transporter)
Gene: SLC22A1
UniProt: O15245 (S22A1_HUMAN)
Organism: Homo sapiens
Activity: IC50 = 4.79
Assay: Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Drug: erlotinib
Target: Ephrin type-B receptor 4 (Kinase)
Gene: EPHB4
UniProt: P54760 (EPHB4_HUMAN)
Organism: Homo sapiens
Activity: Kd = 5.66
Assay: Binding constant for EPHB4 kinase domain