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TargetCytochrome P450 3A4(Human)
Cytokinetics

Curated by ChEMBL
LigandPNGBDBM50575174(Mavacamten)
Affinity DataEC50:  2.20E+3nMAssay Description:Induction of CYP3A4 in human hepatocytes assessed as mRNA expression incubated for 3 days by RT-RTPCR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 2B6(Human)
Cytokinetics

Curated by ChEMBL
LigandPNGBDBM50575174(Mavacamten)
Affinity DataEC50:  5.10E+3nMAssay Description:Induction of CYP2B6 in human hepatocytes assessed as mRNA expression incubated for 3 days by RT-RTPCR analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276129((2S,4bR,8aR)-4b-Ethyl-7-phenyl-4b,5,6,7,8,8a,9,10-...)
Affinity DataIC50: 1.30nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276127((2R,3S,4aR,10aR)-4a-Ethyl-7-(2-methylpyridin-3-ylm...)
Affinity DataIC50: 1.5nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276434((2R,4aR,10aR)-4a-Propyl-2-prop-1-ynyl-1,2,3,4,4a,9...)
Affinity DataIC50: 1.5nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276438((2R,4aR,10aR)-4a-Ethyl-7-(2-methylpyridin-3-ylmeth...)
Affinity DataIC50: 2.30nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276126((2R,3S,4aR,10aR)-4a-Ethyl-2-phenyl-1,2,3,4,4a,9,10...)
Affinity DataIC50: 2.5nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276437((2R,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-7-(pyridin-4-...)
Affinity DataIC50: 3nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276472((2R,3S,4aR,10aR)-4a-Ethyl-7-(2-methylpyridin-3-ylm...)
Affinity DataIC50: 3.30nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276171((2R,4aS,10aR)-4a-Propenyl-2-prop-1-ynyl-1,2,3,4,4a...)
Affinity DataIC50: 3.5nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276128((2R,3R,4aR,10aR)-4a-Ethyl-2-phenyl-1,2,3,4,4a,9,10...)
Affinity DataIC50: 3.80nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276170((2R,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 5.60nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276475((2R,4aR,10aR)-4a-Ethyl-7-(2-methylpyridin-3-ylmeth...)
Affinity DataIC50: 6nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276168((2R,4aR,10aR)-4a-Allyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 6.20nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276438((2R,4aR,10aR)-4a-Ethyl-7-(2-methylpyridin-3-ylmeth...)
Affinity DataIC50: 6.30nMAssay Description:Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276170((2R,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 14nMAssay Description:Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276168((2R,4aR,10aR)-4a-Allyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 14nMAssay Description:Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276472((2R,3S,4aR,10aR)-4a-Ethyl-7-(2-methylpyridin-3-ylm...)
Affinity DataIC50: 15nMAssay Description:Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 3A4(Human)
Cytokinetics

Curated by ChEMBL
LigandPNGBDBM151585(US8987315, Ketoconazole | US9180183, Ketoconazole ...)
Affinity DataIC50: 15nMAssay Description:Inhibition of CYP3A4 using in human liver microsomes using testosterone as substrate after 5 to 15 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276169((2R,4aR,10aR)-4a-Methyl-2-prop-1-ynyl-1,2,3,4,4a,9...)
Affinity DataIC50: 17nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 3A4(Human)
Cytokinetics

Curated by ChEMBL
LigandPNGBDBM151585(US8987315, Ketoconazole | US9180183, Ketoconazole ...)
Affinity DataIC50: 18nMAssay Description:Inhibition of CYP3A4 using in human liver microsomes using midazolam as substrate after 5 to 15 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276474((2R,4aR,10aR)-4a-Ethyl-2-phenyl-1,2,3,4,4a,9,10,10...)
Affinity DataIC50: 21nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276437((2R,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-7-(pyridin-4-...)
Affinity DataIC50: 31nMAssay Description:Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276168((2R,4aR,10aR)-4a-Allyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 34nMAssay Description:Transrepression activity at GR in human SW1353 cells assessed as suppression of NFkappaB-induced IL8 productionMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276471((2R,3S,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-1,2,3,4,4a...)
Affinity DataIC50: 35nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 2D6(Human)
Global Blood Therapeutics

Curated by ChEMBL
LigandPNGBDBM50121975((6-Methoxy-quinolin-4-yl)-(5-vinyl-1-aza-bicyclo[2...)
Affinity DataIC50: 35nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate after 5 to 15 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276127((2R,3S,4aR,10aR)-4a-Ethyl-7-(2-methylpyridin-3-ylm...)
Affinity DataIC50: 38nMAssay Description:Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 1A2(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50348420(CHEMBL1800951)
Affinity DataIC50: 60nMAssay Description:Inhibition of CYP1A2More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276471((2R,3S,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-1,2,3,4,4a...)
Affinity DataIC50: 63nMAssay Description:Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 1A2(Human)
TBA

Curated by ChEMBL
LigandPNGBDBM50348418(CHEMBL1800931)
Affinity DataIC50: 80nMAssay Description:Inhibition of CYP1A2More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetEstrogen receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276170((2R,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 89nMAssay Description:Binding affinity to human ERalphaMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetEstrogen receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276168((2R,4aR,10aR)-4a-Allyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 93nMAssay Description:Binding affinity to human ERalphaMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276126((2R,3S,4aR,10aR)-4a-Ethyl-2-phenyl-1,2,3,4,4a,9,10...)
Affinity DataIC50: 140nMAssay Description:Transrepression activity at GR in human SW1353 cells assessed as inhibition of IL1-stimulated MMP13 production after 24 hrs by whole cell ELISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 2C9(Human)
Global Blood Therapeutics

Curated by ChEMBL
LigandPNGBDBM50090677(CHEMBL1109 | 4-Amino-N-(2-phenyl-2H-pyrazol-3-yl)-...)
Affinity DataIC50: 205nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using tolbutamide as substrate after 5 to 15 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetEstrogen receptor beta(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276168((2R,4aR,10aR)-4a-Allyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 250nMAssay Description:Binding affinity to human ERbetaMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276473((2S,4R,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-1,2,3,4,4a...)
Affinity DataIC50: 360nMAssay Description:Binding affinity to human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetAndrogen receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276170((2R,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 420nMAssay Description:Binding affinity to human androgen receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetEstrogen receptor beta(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276170((2R,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-1,2,3,4,4a,9,...)
Affinity DataIC50: 580nMAssay Description:Binding affinity to human ERbetaMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM691025((R)-N-(5-(5-ethylisoxazol-3-yl)-2,3- dihydro-1H-in...)
Affinity DataIC50: 600nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM691028(US12065436, Compound 417 | (R)-N-(5-(5-ethylisoxaz...)
Affinity DataIC50: 600nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM691035(US12065436, Compound 424 | (S)-N-(6-(5-ethylisoxaz...)
Affinity DataIC50: 600nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM691175(US12065436, Compound 564 | (R)-N-(5-(5-ethyl-1,2,4...)
Affinity DataIC50: 600nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM691231(US12065436, Compound 620 | (R)-3-chloro-N-(5-(5-et...)
Affinity DataIC50: 600nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetEstrogen receptor beta(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276126((2R,3S,4aR,10aR)-4a-Ethyl-2-phenyl-1,2,3,4,4a,9,10...)
Affinity DataIC50: 660nMAssay Description:Binding affinity to human ERbetaMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetEstrogen receptor(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50276437((2R,4aR,10aR)-4a-Ethyl-2-prop-1-ynyl-7-(pyridin-4-...)
Affinity DataIC50: 670nMAssay Description:Binding affinity to human ERalphaMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM690915(methyl (R)-(5-(5-ethyl-1,2,4- oxadiazol-3-yl)-2,3-...)
Affinity DataIC50: 700nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM690951((S)-N-(6-(5-ethyl-1,2,4-oxadiazol-3- yl)-2,3-dihyd...)
Affinity DataIC50: 700nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM691020((R)-N-(5-(5-cyclobutyl-1,2,4- oxadiazol-3-yl)-2,3-...)
Affinity DataIC50: 700nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM691064(US12065436, Compound 453 | (S)-N-(6-(5-(difluorome...)
Affinity DataIC50: 700nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

TargetMyosin-1(Bovine)
CYTOKINETICS, INC.

US Patent
LigandPNGBDBM691066(US12065436, Compound 455 | (S)-N-(6-(5-ethyl-1,2,4...)
Affinity DataIC50: 700nMAssay Description:To evaluate the effect of compounds on the ATPase activity of full-length cardiac myosin in the context of the native sarcomere, skinned myofibril as...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails
US Patent

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