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ChEMBL ligand: CHEMBL411 (Apstil, Cyren a, Diethylstilbestrol, Distilbene, Estrobene, Estrogenine, Estromenin, Fonatol, New-estranol 1, NSC-3070, Palestrol, Stilbestro, Stilbestroform, Stilbestrol, Stilbetin, Stilboesterol, Stilboestrol, Synestrin, Synthestrin, Tampovagan) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
ChEMBL | DRUGMATRIX: Acetylcholinesterase enzyme inhibition (substrate: acetylthiocholine) | B | 4.59 | pIC50 | 25550 | nM | IC50 | DrugMatrix in vitro pharmacology data |
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) | B | 5.78 | pKi | 1666 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) | B | 5.54 | pIC50 | 2856 | nM | IC50 | DrugMatrix in vitro pharmacology data |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 5.3 | pKi | 5060 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 5.05 | pIC50 | 9013 | nM | IC50 | DrugMatrix in vitro pharmacology data |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 5.9 | pKi | 1248 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 5.66 | pIC50 | 2208 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.1 | pKi | 7888 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) | B | 4.71 | pIC50 | 19487 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.27 | pKi | 5321 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 4.97 | pIC50 | 10826 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 5.28 | pKi | 5297 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 4.85 | pIC50 | 14127 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 5.27 | pKi | 5340 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 4.93 | pIC50 | 11698 | nM | IC50 | DrugMatrix in vitro pharmacology data |
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 5.66 | pKi | 2201 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) | B | 4.82 | pIC50 | 15151 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
ChEMBL | Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) | B | 4.85 | pIC50 | 14125.38 | nM | IC50 | J Med Chem (2005) 48: 5666-5674 [PMID:16134935] |
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530] | ||||||||
ChEMBL | DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) | B | 5.53 | pIC50 | 2963 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
ChEMBL | TP_TRANSPORTER: drug resistance(Mitoxantrone) in BCRP-expressing K562 cells | F | 6.3 | pIC50 | 500 | nM | IC50 | Mol Cancer Ther (2003) 2: 105-112 [PMID:12533678] |
ChEMBL | TP_TRANSPORTER: drug resistance(SN-38) in BCRP-expressing K562 cells | F | 6.3 | pIC50 | >500 | nM | IC50 | Mol Cancer Ther (2003) 2: 105-112 [PMID:12533678] |
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 4.89 | pKi | 12755 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 4.66 | pIC50 | 22088 | nM | IC50 | DrugMatrix in vitro pharmacology data |
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
ChEMBL | DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) | B | 5.25 | pIC50 | 5600 | nM | IC50 | DrugMatrix in vitro pharmacology data |
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271] | ||||||||
ChEMBL | DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) | B | 5.05 | pKi | 8872 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4) | B | 4.75 | pIC50 | 17745 | nM | IC50 | DrugMatrix in vitro pharmacology data |
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 6.02 | pKi | 958 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole) | B | 5.57 | pIC50 | 2718 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 5.41 | pKi | 3882 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 5.11 | pIC50 | 7763 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 5.35 | pKi | 4440 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) | B | 4.88 | pIC50 | 13321 | nM | IC50 | DrugMatrix in vitro pharmacology data |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 5.52 | pKi | 2987 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) | B | 5.06 | pIC50 | 8796 | nM | IC50 | DrugMatrix in vitro pharmacology data |
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 6.07 | pKi | 851 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.97 | pIC50 | 1071 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
ChEMBL | In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor alpha | B | 9.31 | pKi | 0.49 | nM | Ki | J Med Chem (2003) 46: 1408-1418 [PMID:12672240] |
ChEMBL | DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) | B | 9.58 | pKi | 0.26 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]Estradiol from human recombinant estrogen receptor alpha expressed in Sf9 cells after 2 hrs | B | 9.66 | pKi | 0.22 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
GtoPdb | - | - | 10.4 | pKi | - | - | - | Endocrinology (1997) 138: 863-70 [PMID:9048584] |
ChEMBL | Displacement of [3H]-estradiol from human recombinant ERalpha expressed in Sf21 cells after 2 hrs | B | 6.11 | pIC50 | 770 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4307-4309 [PMID:22652053] |
ChEMBL | In vitro inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2001) 44: 1654-1657 [PMID:11356100] |
ChEMBL | DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol) | B | 9.04 | pIC50 | 0.92 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of [3H]Estradiol from human recombinant estrogen receptor alpha expressed in Sf9 cells after 2 hrs | B | 9.11 | pIC50 | 0.77 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Displacement of radioligand from Estrogen receptor alpha | B | 9.48 | pIC50 | 0.33 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1283-1285 [PMID:11965371] |
ChEMBL | Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor alpha. | B | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (2002) 45: 1399-1401 [PMID:11906280] |
ChEMBL | Agonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ER-alpha-mediated transcriptional activity by luciferase reporter gene assay | B | 9.7 | pEC50 | 0.2 | nM | EC50 | Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565] |
ChEMBL | Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay | B | 9.96 | pEC50 | 0.11 | nM | EC50 | Bioorg Med Chem (2019) 27: 1952-1961 [PMID:30940565] |
ChEMBL | Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha. | B | 10.22 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2002) 45: 1399-1401 [PMID:11906280] |
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
ChEMBL | In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor beta | B | 9.2 | pKi | 0.63 | nM | Ki | J Med Chem (2003) 46: 1408-1418 [PMID:12672240] |
GtoPdb | - | - | 9.8 | pKi | - | - | - | Endocrinology (1997) 138: 863-70 [PMID:9048584] |
ChEMBL | Displacement of [3H]-estradiol from human recombinant ERbeta expressed in Sf21 cells after 2 hrs | B | 6.21 | pIC50 | 610 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4307-4309 [PMID:22652053] |
ChEMBL | In vitro inhibitory concentration against [3H]17-beta-estradiol binding to human estrogen receptor 2 | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2001) 44: 1654-1657 [PMID:11356100] |
ChEMBL | Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor beta. | B | 8.05 | pEC50 | 9 | nM | EC50 | J Med Chem (2002) 45: 1399-1401 [PMID:11906280] |
ChEMBL | Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta. | B | 10.7 | pEC50 | 0.02 | nM | EC50 | J Med Chem (2002) 45: 1399-1401 [PMID:11906280] |
Estrogen-related receptor-γ/Estrogen-related receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4245] [GtoPdb: 624] [UniProtKB: P62508] | ||||||||
GtoPdb | - | - | 5.3 | pIC50 | - | - | - |
Genes Dev (2001) 15: 833-8 [PMID:11297507]; Proc Natl Acad Sci USA (2001) 98: 8880-4 [PMID:11447273] |
ChEMBL | Estrogen-Related Receptor gamma activity in FRET assay | F | 6.2 | pEC50 | 630 | nM | EC50 | J Med Chem (2005) 48: 3107-3109 [PMID:15857113] |
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 5.32 | pKi | 4818 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 4.97 | pIC50 | 10600 | nM | IC50 | DrugMatrix in vitro pharmacology data |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.74 | pKi | 1825 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.34 | pIC50 | 4563 | nM | IC50 | DrugMatrix in vitro pharmacology data |
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
ChEMBL | DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein) | B | 4.48 | pIC50 | 32903 | nM | IC50 | DrugMatrix in vitro pharmacology data |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.63 | pKi | 2345 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 5.24 | pIC50 | 5778 | nM | IC50 | DrugMatrix in vitro pharmacology data |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.44 | pKi | 3654 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 4.82 | pIC50 | 15171 | nM | IC50 | DrugMatrix in vitro pharmacology data |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 5.41 | pKi | 3907 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 4.73 | pIC50 | 18432 | nM | IC50 | DrugMatrix in vitro pharmacology data |
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
ChEMBL | DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) | B | 5.5 | pKi | 3184 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) | B | 5.02 | pIC50 | 9553 | nM | IC50 | DrugMatrix in vitro pharmacology data |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.44 | pKi | 3640 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.44 | pIC50 | 3670 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
ChEMBL | Antagonist activity at full length human PXR transfected in human HepG2 cells assessed as reduction in rifaximin-induced receptor transactivation after 18 hrs by luciferase reporter assay | B | 4.84 | pIC50 | 14600 | nM | IC50 | Eur J Med Chem (2015) 103: 551-562 [PMID:26408814] |
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] | ||||||||
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 6.21 | pKi | 611 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 5.33 | pIC50 | 4682 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191] | ||||||||
ChEMBL | Inhibition of rabbit microsomes SERCA1a by enzyme-coupled method | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2020) 63: 1937-1963 [PMID:32030976] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 5.86 | pKi | 1369 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) | B | 5.32 | pIC50 | 4790 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.7 | pKi | 1998 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.5 | pIC50 | 3140 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 4.57 | pKi | 26619 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 4.29 | pIC50 | 50819 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 5.22 | pKi | 5986 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) | B | 4.89 | pIC50 | 12892 | nM | IC50 | DrugMatrix in vitro pharmacology data |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.18 | pKi | 6637 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 4.9 | pIC50 | 12492 | nM | IC50 | DrugMatrix in vitro pharmacology data |
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557] | ||||||||
ChEMBL | DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) | B | 5.36 | pIC50 | 4359 | nM | IC50 | DrugMatrix in vitro pharmacology data |
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
ChEMBL | DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) | B | 4.85 | pIC50 | 14233 | nM | IC50 | DrugMatrix in vitro pharmacology data |
UDP-glucose 4-epimerase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5843] [UniProtKB: Q14376] | ||||||||
ChEMBL | Inhibition of human GalE by HPAEC assay | B | 4.12 | pIC50 | 75000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5744-5747 [PMID:16962325] |
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
ChEMBL | DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr) | B | 4.98 | pKi | 10401 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr) | B | 4.59 | pIC50 | 25925 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Estrogen-related receptor-α in Mouse [GtoPdb: 622] [UniProtKB: O08580] | ||||||||
GtoPdb | - | - | 5.3 | pIC50 | - | - | - | Genes Dev (2001) 15: 833-8 [PMID:11297507] |
Estrogen-related receptor-β in Human [GtoPdb: 623] [UniProtKB: O95718] | ||||||||
GtoPdb | - | - | 5.3 | pIC50 | - | - | - | Genes Dev (2001) 15: 833-8 [PMID:11297507] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]