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Assay Detail

CHEMBL4034784

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

Binding
Inhibition of ERK phosphorylation in human MDA-MB-231 cells after 1 hr
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of tetrahydrocarbazoles as dual pERK and pRb inhibitors.
Kulkarni MR, Mane MS, Ghosh U, Sharma R, Lad NP, Srivastava A, Kulkarni-Almeida A, Kharkar PS, Khedkar VM, Pandit SS.
Eur J Med Chem (2017) 134 : 366 -378
PubMed 28431342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.17 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1336 SORAFENIB 4.0 1 7.20
CHEMBL4065808 1 5.52
CHEMBL4075216 1 5.52
CHEMBL4077816 1 5.44
CHEMBL4068198 1 5.36
CHEMBL4070208 1 5.34
CHEMBL4086582 1 5.26
CHEMBL4068744 1 5.26
CHEMBL4070561 1 5.26
CHEMBL4092194 1 5.22
CHEMBL4061653 1 5.21
CHEMBL4064772 1 5.16
CHEMBL4083343 1 5.16
CHEMBL4075949 1 5.12
CHEMBL4060594 1 5.09
CHEMBL4077480 1 5.05
CHEMBL4071674 1 5.05
CHEMBL4092469 1 4.68
CHEMBL4075814 1 4.68
CHEMBL4082197 1 4.53
CHEMBL4093413 1 4.52
CHEMBL4063962 1 4.16
CHEMBL4067615 1 -
CHEMBL4088842 1 -
CHEMBL4094137 1 -
CHEMBL4076325 1 -
CHEMBL4082537 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1336 SORAFENIB IC50 = 63.0 nM 7.20
CHEMBL4065808 IC50 = 3000.0 nM 5.52
CHEMBL4075216 IC50 = 3000.0 nM 5.52
CHEMBL4077816 IC50 = 3620.0 nM 5.44
CHEMBL4068198 IC50 = 4400.0 nM 5.36
CHEMBL4070208 IC50 = 4600.0 nM 5.34
CHEMBL4086582 IC50 = 5500.0 nM 5.26
CHEMBL4068744 IC50 = 5520.0 nM 5.26
CHEMBL4070561 IC50 = 5500.0 nM 5.26
CHEMBL4092194 IC50 = 6000.0 nM 5.22
CHEMBL4061653 IC50 = 6110.0 nM 5.21
CHEMBL4064772 IC50 = 7000.0 nM 5.16
CHEMBL4083343 IC50 = 7000.0 nM 5.16
CHEMBL4075949 IC50 = 7500.0 nM 5.12
CHEMBL4060594 IC50 = 8100.0 nM 5.09
CHEMBL4077480 IC50 = 9000.0 nM 5.05
CHEMBL4071674 IC50 = 9000.0 nM 5.05
CHEMBL4092469 IC50 = 21000.0 nM 4.68
CHEMBL4075814 IC50 = 21000.0 nM 4.68
CHEMBL4082197 IC50 = 29680.0 nM 4.53
CHEMBL4093413 IC50 = 30000.0 nM 4.52
CHEMBL4063962 IC50 = 69860.0 nM 4.16
CHEMBL4067615 IC50 > 100000.0 nM -
CHEMBL4088842 IC50 > 30000.0 nM -
CHEMBL4094137 IC50 > 100000.0 nM -
CHEMBL4076325 IC50 > 100000.0 nM -
CHEMBL4082537 IC50 > 100000.0 nM -