PLX-4720 - Small Molecule (ID:10049-101)

HMS LINCS ID: 10049-101
Name: PLX-4720
Alternative Names:
LINCS ID: LSM-1049
PubChem CID: 24180719
ChEBI ID:
ChEMBL ID:
Molecular Mass: 413.04
InChi: InChI=1S/C17H14ClF2N3O3S/c1-2-5-27(25,26)23-13-4-3-12(19)14(15(13)20)16(24)11-8-22-17-10(11)6-9(18)7-21-17/h3-4,6-8,23H,2,5H2,1H3,(H,21,22)
InChi Key: YZDJQTHVDDOVHR-UHFFFAOYSA-N
SMILES: CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=NC=C(C=C23)Cl)F
Relevant Citations:
Comments:
Date Publicly Available:
Most Recent Update: 2016-04-04

Target Affinity:

(see Study 20000)
Target Affinity Spectrum Value HUGO Gene Name
1
(Kd <100 nM)
FGR, MAP2K5, MAP3K20, PF3D7_0217500, PTK6, RAF1, SRMS
2
(equivalent to 100 nM ≤ Kd < 1µM)
BRAF, CDK19, EPHB6, LIMK2, MAP2K1, MAP2K4, NEK11, PDGFRA, PDGFRB, RIOK2, RIPK2, SIK1, SIK1B, TGFBR2
3
(equivalent to 1µM ≤ Kd < 10 µM)
ABL1, ABL2, ACVR2B, AIM1, AURKB, AURKC, BLK, BMPR1B, C8orf44-SGK3, CAMK1, CDK8, CLK1, CLK2, CSF1R, CSK, CSNK1G2, DCLK1, DCLK3, DDR1, DDR2, DYRK2, EIF2AK4, FES, FGFR1, FGFR2, FLG, FLT1, FLT3, FRK, FYN, HCK, HIPK1, HIPK2, HIPK3, HIPK4, KDR, KIT, LCK, LIMK1, LYN, MAP2K2, MAP4K5, MINK1, MYLK4, NEK2, OSR1, OXSR1, PAK1, PI4KB, PLK4, RIPK1, SGK3, SIK2, SLK, SRC, STK16, STK36, TESK1, TKT, TNIK, TNK2, YES1
10
(confirmed non-binding)
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Datasets:

HMS Dataset ID Dataset Title HMS Dataset Type
20000
Target Affinity Spectrum (TAS) vectors for compounds in the HMS LINCS small molecule library.
Analysis
20024
PLX-4720 KINOMEscan
 KINOMEscan
20090
PLX-4720 KiNativ -- dose response experiment
 KiNativ
20217
Viability and apoptosis in BRAF(V600E/D) melanoma cell lines monitored by imaging
 Microscopy/Imaging
20218
Phosphorylation state and protein levels measured in BRAF(V600E/D) melanoma cell lines monitored by Reverse Phase Protein Arrays (RPPA)
 Reverse Phase Protein Array
20237
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 1 of 15: Cell count and relative growth within biological replicate 1.
 Microscopy/Imaging
20238
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 2 of 15: Cell count and relative growth within biological replicate 2.
 Microscopy/Imaging
20239
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 3 of 15: Cell count and relative growth within biological replicate 3.
 Microscopy/Imaging
20240
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 4 of 15: Mean cell count and mean growth rate across biological replicate 1.
 Microscopy/Imaging
20241
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 5 of 15: Mean cell count and mean growth rate across biological replicate 2.
 Microscopy/Imaging
20242
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 6 of 15: Mean cell count and mean growth rate across biological replicate 3.
 Microscopy/Imaging
20243
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 7 of 15: Mean cell count and mean growth rate across all replicates.
 Microscopy/Imaging
20245
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 8 of 15: Cell count and normalized growth rate inhibition values within biological replicate 1.
 Microscopy/Imaging
20246
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 9 of 15: Cell count and normalized growth rate inhibition values within biological replicate 2.
 Microscopy/Imaging
20247
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 10 of 15: Cell count and normalized growth rate inhibition values within biological replicate 3.
 Microscopy/Imaging
20248
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 11 of 15: Mean cell count and mean normalized growth rate inhibition values across biological replicate 1.
 Microscopy/Imaging
20249
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 12 of 15: Mean cell count and mean normalized growth rate inhibition values across biological replicate 2.
 Microscopy/Imaging
20250
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 13 of 15: Mean cell count and mean normalized growth rate inhibition values across biological replicate 3.
 Microscopy/Imaging
20251
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 14 of 15: Mean cell count and mean normalized growth rate inhibition values across all replicates.
 Microscopy/Imaging
20252
LINCS Pilot Phase Joint Project: Sensitivity measures of six breast cancer cell lines to a library of small molecule kinase inhibitors (single drug treatments). Dataset 15 of 15: Calculated dose-response metrics.
 Analysis
20256
Breast Cancer Cell Density: Imaging assay of the density- and context-dependence of small molecule perturbagen response in breast cancer cell lines. Dataset 1 of 3: Cell count and normalized growth rate inhibition values.
 Microscopy/Imaging
20257
Breast Cancer Cell Density: Imaging assay of the density- and context-dependence of small molecule perturbagen response in breast cancer cell lines. Dataset 2 of 3: Mean cell count and mean normalized growth rate inhibition values across all replicates.
 Microscopy/Imaging
20258
Breast Cancer Cell Density: Imaging assay of the density- and context-dependence of small molecule perturbagen response in breast cancer cell lines. Dataset 3 of 3: Calculated dose-response metrics.
 Analysis

KINOMEscan Image

Batch Information:

HMS LINCS Batch ID Provider Provider Batch ID
10049-101-1 Nathanael Gray (DFCI) PLX-4720-1