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Found 4799 with Last Name = 'newhouse' and Initial = 'b'
TargetGTPase KRas(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM50503649(CHEMBL4476113)
Affinity DataKi:  2.00E+5nMAssay Description:Inhibition of KRAS G12C mutant (unknown origin)More data for this Ligand-Target Pair
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM617349(US20230279025, Example 465)
Affinity DataIC50:  0.00100nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM617355(US20230279025, Example 468)
Affinity DataIC50: <0.00200nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579601(CHEMBL4858364 | US11453683, Example 252 | US202302...)
Affinity DataIC50: <0.00200nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM617323(US20230279025, Example 452 | US20230279025, Exampl...)
Affinity DataIC50: <0.00200nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM617363(US20230279025, Example 482)
Affinity DataIC50: <0.00200nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM617357(US20230279025, Example 469)
Affinity DataIC50: <0.00200nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM573400(US11453683, Example 259 | US20230279025, Example 4...)
Affinity DataIC50: <0.00200nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM617351(US20230279025, Example 466)
Affinity DataIC50:  0.00600nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM617347(US20230279025, Example 464)
Affinity DataIC50:  0.00700nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM617345(US20230279025, Example 463)
Affinity DataIC50:  0.0120nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25619((1Z)-5-[1-methyl-3-(pyridin-4-yl)-1H-pyrazol-4-yl]...)
Affinity DataIC50:  0.0200nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM617339(US20230279025, Example 460)
Affinity DataIC50:  0.0270nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25636((1Z)-5-[1-(piperidin-4-yl)-3-(pyridin-4-yl)-1H-pyr...)
Affinity DataIC50:  0.0300nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25625((1S,3R)-3-{4-[(1Z)-1-(hydroxyimino)-2,3-dihydro-1H...)
Affinity DataIC50:  0.0400nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25629(3-{4-[(1Z)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5...)
Affinity DataIC50:  0.0500nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM616938(US20230279025, Example 26 | US20230279025, Example...)
Affinity DataIC50:  0.0620nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25626((1R,3R)-3-{4-[(1Z)-1-(hydroxyimino)-2,3-dihydro-1H...)
Affinity DataIC50:  0.0900nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM573426(US11453683, Example 284 | US20230279025, Example 2...)
Affinity DataIC50:  0.100nMAssay Description:Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KR...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM573426(US11453683, Example 284 | US20230279025, Example 2...)
Affinity DataIC50:  0.100nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25628(2-{4-[(1Z)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5...)
Affinity DataIC50:  0.130nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25618((1Z)-5-[3-(pyridin-4-yl)-1H-pyrazol-4-yl]-2,3-dihy...)
Affinity DataIC50:  0.150nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579600(CHEMBL4857438 | US11453683, Example 251 | US202302...)
Affinity DataIC50:  0.200nMAssay Description:Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KR...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM50484212(CHEMBL1822264)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of full length B-Raf V600E mutantMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579600(CHEMBL4857438 | US11453683, Example 251 | US202302...)
Affinity DataIC50:  0.200nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25638((1Z)-5-[1-(oxan-4-yl)-3-(pyridin-4-yl)-1H-pyrazol-...)
Affinity DataIC50:  0.220nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25641(3-{4-[(1Z)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5...)
Affinity DataIC50:  0.230nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579595(CHEMBL4863339 | US11453683, Example 185 | US202302...)
Affinity DataIC50:  0.300nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579595(CHEMBL4863339 | US11453683, Example 185 | US202302...)
Affinity DataIC50:  0.300nMAssay Description:Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KR...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25624((1R,2R)-2-{4-[(1Z)-1-(hydroxyimino)-2,3-dihydro-1H...)
Affinity DataIC50:  0.330nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25637((1Z)-5-[1-(1-methylpiperidin-4-yl)-3-(pyridin-4-yl...)
Affinity DataIC50:  0.340nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf [V600E](Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM565148(US11414404, Ex. # 25 | US11634409, Example 25)
Affinity DataIC50:  0.340nMAssay Description:A competitive displacement assay was configured for B-Raf that monitors the amount of a fluorescently-tagged “tracer” bound to B-Raf via TR-FRET from...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase B-raf [V600E](Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM565148(US11414404, Ex. # 25 | US11634409, Example 25)
Affinity DataIC50:  0.340nMAssay Description:A competitive displacement assay was configured for B-Raf that monitors the amount of a fluorescently-tagged “tracer” bound to B-Raf via TR-FRET from...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetEstrogen receptor beta(RAT)
Pfizer

Curated by ChEMBL
LigandPNGBDBM17292((1S,10R,11S,14S,15S)-15-methyltetracyclo[8.7.0.0^{...)
Affinity DataIC50:  0.354nMAssay Description:Inhibition of estradiol binding to estrogen receptorMore data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM25634(3-{4-[(1Z)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5...)
Affinity DataIC50:  0.390nMpH: 7.2 T: 2°CAssay Description:Activity of human recombinant B-Raf protein was assessed in vitro by assay of the incorporation of radiolabeled phosphate to recombinant MAP kinase (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase B-raf(Homo sapiens (Human))
Array Biopharma

LigandPNGBDBM50485033(CHEMBL2023502)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of full-length B-Raf V600E mutant assessed as reduction in incorporation of radiolabeled phosphate from [gamma-33P]ATP into FSBA-modified ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579601(CHEMBL4858364 | US11453683, Example 252 | US202302...)
Affinity DataIC50:  0.400nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579594(CHEMBL4859236 | US11453683, Example 36 | US2023027...)
Affinity DataIC50:  0.400nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579597(CHEMBL4876040 | US11453683, Example 243 | US202302...)
Affinity DataIC50:  0.400nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetMitogen-activated protein kinase 1 [8-360](Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM193676(US9670208, Example 295 4-(3-(cyclopropylmethyl)-[1...)
Affinity DataIC50:  0.400nMpH: 7.3Assay Description:Compounds were tested in an enzymatic assay using human ERK-2 (Mitogen Activated Kinase 1), recombinantly expressed as an n-terminal 6-His fusion pro...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM573433(US11453683, Example 63 | US20230279025, Example 63)
Affinity DataIC50:  0.400nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM573644(US11453683, Example 439 | US20230279025, Example 4...)
Affinity DataIC50:  0.400nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM573484(US11453683, Example 340 | US20230279025, Example 3...)
Affinity DataIC50:  0.400nMAssay Description:This Example illustrates that exemplary compounds of the present invention inhibit the phosphorylation of ERK downstream of KRAS G12D. AGS cells (ATC...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM573644(US11453683, Example 439 | US20230279025, Example 4...)
Affinity DataIC50:  0.400nMAssay Description:Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KR...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM573433(US11453683, Example 63 | US20230279025, Example 63)
Affinity DataIC50:  0.400nMAssay Description:Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KR...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM573484(US11453683, Example 340 | US20230279025, Example 3...)
Affinity DataIC50:  0.400nMAssay Description:Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KR...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579597(CHEMBL4876040 | US11453683, Example 243 | US202302...)
Affinity DataIC50:  0.400nMAssay Description:Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KR...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579601(CHEMBL4858364 | US11453683, Example 252 | US202302...)
Affinity DataIC50:  0.400nMAssay Description:Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KR...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGTPase KRas [G12D](Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM50579594(CHEMBL4859236 | US11453683, Example 36 | US2023027...)
Affinity DataIC50:  0.400nMAssay Description:Table 2: The ability of a compound to bind to KRAS G12D was measured using a TR-FRET displacement assay. Biotinylated GDP-loaded recombinant human KR...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSerine/threonine-protein kinase B-raf [V600E](Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM565192(US11414404, Ex. # 69 | US11634409, Example 69)
Affinity DataIC50:  0.460nMAssay Description:A competitive displacement assay was configured for B-Raf that monitors the amount of a fluorescently-tagged “tracer” bound to B-Raf via TR-FRET from...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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