NanoBRET layout3 outlineのコピー · Carna Biosciences, Inc. 0 10 20 30 40 0 2 4 6 8 10 12 14 16...
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Carna Biosciences, Inc. 0 10 20 30 40 0 2 4 6 8 10 12 14 16 18 20 BRET Ratio (mBRET) Time (min) DMSO Palbociclib Ribociclib Abemaciclib K-7 K-10 0 5 10 15 20 25 30 0 2 4 6 8 10 12 14 16 18 20 BRET Ratio (mBRET) Time (min) DMSO Palbociclib Ribociclib Abemaciclib 0 10 20 30 40 50 0 2 4 6 8 10 12 14 16 18 20 BRET Ratio (mBRET) Time (min) DMSO Dinaciclib NVP-2 0 5 10 15 20 0 2 4 6 8 10 12 14 16 18 20 BRET Ratio (mBRET) Time (min) DMSO Dinaciclib NVP-2 0.001 0.01 0.1 1 10 0.001 0.01 0.1 1 k d in K-5 assay (min -1 ) k d in K-4 assay (min -1 ) r 2 = 0.0146 Fenebrutinib Ibrutinib Acalabrutinib Zanubrutinib 0.001 0.01 0.1 1 0.001 0.01 0.1 1 k d in K-5 assay (min -1 ) k d in K-4 assay (min -1 ) r 2 = 0.8655 Fenebrutinib Ibrutinib Acalabrutinib Zanubrutinib 0.01 0.1 1 0.01 0.1 1 k d in K-10 assay (min -1 ) k d in K-7 or K-8 assay (min -1 ) r 2 = 0.7632 Palbociclib NVP-2 0.01 0.1 1 0.01 0.1 1 k d in K-10 assay (min -1 ) k d in K-7 or K-8 assay (min -1 ) r 2 = 0.7504 Palbociclib NVP-2 [RL] Imax [RL] I=0 = {(1-exp(-k obs ×t))/k obs + (exp(-k obs ×t)-exp(-k d ×t))/(k obs -k d )} (1-exp(-k obs ×t))/k obs 0 20 40 60 80 100 120 0 20 40 60 80 100 120 BRET Ratio (mBRET) Time (min) DMSO Dasatinib Ibrutinib Fenebrutinib Acalabrutinib Zanubrutinib CGI-1746 RN-486 Vecabrutinib ARQ-531 0 10 20 30 40 50 0.0 1.6 3.2 4.8 6.4 BRET Ratio (mBRET) Time (min) DMSO Ibrutinib Fenebrutinib Acalabrutinib Zanubrutinib 0 10 20 30 40 50 0.0 1.6 3.2 4.8 6.4 BRET Ratio (mBRET) Time (min) DMSO Dasatinib CGI-1746 RN-486 Vecabrutinib ARQ531
Transcript of NanoBRET layout3 outlineのコピー · Carna Biosciences, Inc. 0 10 20 30 40 0 2 4 6 8 10 12 14 16...
Carna Biosciences, Inc.
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k din
K-5
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ay (m
in-1
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kd in K-4 assay (min-1)
r2 = 0.0146
Fenebrutinib Ibrutinib Acalabrutinib
Zanubrutinib
0.001
0.01
0.1
1
0.001 0.01 0.1 1
k din
K-5
ass
ay (m
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kd in K-4 assay (min-1)
r2 = 0.8655
Fenebrutinib
Ibrutinib
AcalabrutinibZanubrutinib
0.01
0.1
1
0.01 0.1 1
k din
K-1
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kd in K-7 or K-8 assay (min-1)
r2 = 0.7632
Palbociclib
NVP-2
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0.1
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k din
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-1)
kd in K-7 or K-8 assay (min-1)
r2 = 0.7504
PalbociclibNVP-2
[RL]Imax
[RL]I=0=
{(1-exp(-kobs×t))/kobs + (exp(-kobs×t)-exp(-kd×t))/(kobs-kd)}
(1-exp(-kobs×t))/kobs
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Zanubrutinib
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(mB
RET
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Time (min)
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Dasatinib
CGI-1746
RN-486
Vecabrutinib
ARQ531
