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Assay Detail

CHEMBL1828155

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to BRAF V600E mutant
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase B-raf (CHEMBL5145)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.
Holladay MW, Campbell BT, Rowbottom MW, Chao Q, Sprankle KG, Lai AG, Abraham S, Setti E, Faraoni R, Tran L, Armstrong RC, Gunawardane RN, Gardner MF, Cramer MD, Gitnick D, Ator MA, Dorsey BD, Ruggeri BR, Williams M, Bhagwat SS, James J.
Bioorg Med Chem Lett (2011) 21 : 5342 -5346
PubMed 21807507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 28 7.17 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1824291 1 7.54
CHEMBL1824075 1 7.52
CHEMBL1824296 1 7.47
CHEMBL1824073 1 7.44
CHEMBL1824078 1 7.42
CHEMBL1824290 1 7.42
CHEMBL1824068 1 7.40
CHEMBL1824072 1 7.34
CHEMBL1824286 1 7.34
CHEMBL1824287 1 7.34
CHEMBL1824289 1 7.32
CHEMBL1824079 1 7.25
CHEMBL1824297 1 7.25
CHEMBL1824293 1 7.24
CHEMBL1824295 1 7.24
CHEMBL1824070 1 7.21
CHEMBL1824288 1 7.17
CHEMBL1824285 1 7.14
CHEMBL1824069 1 7.14
CHEMBL1824294 1 7.09
CHEMBL1824074 1 7.05
CHEMBL1824076 1 7.02
CHEMBL1824292 1 7.02
CHEMBL1824077 1 7.01
CHEMBL1824080 1 7.00
CHEMBL1336 SORAFENIB 4.0 1 6.55
CHEMBL1277253 1 6.43
CHEMBL1824071 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1824291 Kd = 29.0 nM 7.54
CHEMBL1824075 Kd = 30.0 nM 7.52
CHEMBL1824296 Kd = 34.0 nM 7.47
CHEMBL1824073 Kd = 36.0 nM 7.44
CHEMBL1824078 Kd = 38.0 nM 7.42
CHEMBL1824290 Kd = 38.0 nM 7.42
CHEMBL1824068 Kd = 40.0 nM 7.40
CHEMBL1824072 Kd = 46.0 nM 7.34
CHEMBL1824286 Kd = 46.0 nM 7.34
CHEMBL1824287 Kd = 46.0 nM 7.34
CHEMBL1824289 Kd = 48.0 nM 7.32
CHEMBL1824079 Kd = 56.0 nM 7.25
CHEMBL1824297 Kd = 56.0 nM 7.25
CHEMBL1824293 Kd = 57.0 nM 7.24
CHEMBL1824295 Kd = 57.0 nM 7.24
CHEMBL1824070 Kd = 61.0 nM 7.21
CHEMBL1824288 Kd = 67.0 nM 7.17
CHEMBL1824285 Kd = 72.0 nM 7.14
CHEMBL1824069 Kd = 73.0 nM 7.14
CHEMBL1824294 Kd = 82.0 nM 7.09
CHEMBL1824074 Kd = 90.0 nM 7.05
CHEMBL1824076 Kd = 96.0 nM 7.02
CHEMBL1824292 Kd = 96.0 nM 7.02
CHEMBL1824077 Kd = 98.0 nM 7.01
CHEMBL1824080 Kd = 99.0 nM 7.00
CHEMBL1336 SORAFENIB Kd = 284.0 nM 6.55
CHEMBL1277253 Kd = 370.0 nM 6.43
CHEMBL1824071 Kd = 478.0 nM 6.32