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Assay Detail

CHEMBL4123591

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

Binding
Inhibition of human full length FASN using [3H]-acetyl-CoA/malonyl-CoA as substrate after 60 mins in presence of NADPH by scintillation proximity assay
ChEMBL ↗
46
Total Activities
46
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

Fatty acid synthase (CHEMBL4158) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.
Lu T, Schubert C, Cummings MD, Bignan G, Connolly PJ, Smans K, Ludovici D, Parker MH, Meyer C, Rocaboy C, Alexander R, Grasberger B, De Breucker S, Esser N, Fraiponts E, Gilissen R, Janssens B, Peeters D, Van Nuffel L, Vermeulen P, Bischoff J, Meerpoel L.
Bioorg Med Chem Lett (2018) 28 : 2159 -2164
PubMed 29779975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.74 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4127623 — — 1 7.70
CHEMBL4126247 — — 1 7.70
CHEMBL4129012 — — 1 7.66
CHEMBL4127804 — — 1 7.64
CHEMBL4127964 — — 1 7.60
CHEMBL4128143 — — 1 7.55
CHEMBL4125752 — — 1 7.55
CHEMBL4128261 — — 1 7.52
CHEMBL4129575 — — 1 7.50
CHEMBL4129431 — — 1 7.48
CHEMBL4126768 — — 1 7.44
CHEMBL4126984 — — 1 7.39
CHEMBL4126126 — — 1 7.38
CHEMBL4126304 — — 1 7.34
CHEMBL4129046 — — 1 7.30
CHEMBL4127608 — — 1 7.29
CHEMBL4127027 — — 1 7.16
CHEMBL4129242 — — 1 7.10
CHEMBL4129240 — — 1 7.08
CHEMBL4126572 — — 1 6.92
CHEMBL4128043 — — 1 6.89
CHEMBL4126610 — — 1 6.85
CHEMBL4129199 — — 1 6.80
CHEMBL4127768 — — 1 6.80
CHEMBL4126910 — — 1 6.77
CHEMBL4129812 — — 1 6.70
CHEMBL4130300 — — 1 6.60
CHEMBL4126387 — — 1 6.52
CHEMBL4125929 — — 1 6.52
CHEMBL4126662 — — 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4127623 — IC50 = 20.0 nM 7.70
CHEMBL4126247 — IC50 = 20.0 nM 7.70
CHEMBL4129012 — IC50 = 22.0 nM 7.66
CHEMBL4127804 — IC50 = 23.0 nM 7.64
CHEMBL4127964 — IC50 = 25.0 nM 7.60
CHEMBL4128143 — IC50 = 28.0 nM 7.55
CHEMBL4125752 — IC50 = 28.0 nM 7.55
CHEMBL4128261 — IC50 = 30.0 nM 7.52
CHEMBL4129575 — IC50 = 32.0 nM 7.50
CHEMBL4129431 — IC50 = 33.0 nM 7.48
CHEMBL4126768 — IC50 = 36.0 nM 7.44
CHEMBL4126984 — IC50 = 41.0 nM 7.39
CHEMBL4126126 — IC50 = 42.0 nM 7.38
CHEMBL4126304 — IC50 = 46.0 nM 7.34
CHEMBL4129046 — IC50 = 50.0 nM 7.30
CHEMBL4127608 — IC50 = 51.0 nM 7.29
CHEMBL4127027 — IC50 = 69.0 nM 7.16
CHEMBL4129242 — IC50 = 79.0 nM 7.10
CHEMBL4129240 — IC50 = 83.0 nM 7.08
CHEMBL4126572 — IC50 = 120.0 nM 6.92
CHEMBL4128043 — IC50 = 130.0 nM 6.89
CHEMBL4126610 — IC50 = 140.0 nM 6.85
CHEMBL4127768 — IC50 = 160.0 nM 6.80
CHEMBL4129199 — IC50 = 160.0 nM 6.80
CHEMBL4126910 — IC50 = 170.0 nM 6.77
CHEMBL4129812 — IC50 = 200.0 nM 6.70
CHEMBL4130300 — IC50 = 250.0 nM 6.60
CHEMBL4126387 — IC50 = 300.0 nM 6.52
CHEMBL4125929 — IC50 = 300.0 nM 6.52
CHEMBL4126662 — IC50 = 300.0 nM 6.52
CHEMBL4130264 — IC50 = 360.0 nM 6.44
CHEMBL4127999 — IC50 = 450.0 nM 6.35
CHEMBL4128858 — IC50 = 460.0 nM 6.34
CHEMBL4127363 — IC50 = 460.0 nM 6.34
CHEMBL4127995 — IC50 = 490.0 nM 6.31
CHEMBL4130221 — IC50 = 550.0 nM 6.26
CHEMBL4127681 — IC50 = 590.0 nM 6.23
CHEMBL4130174 — IC50 = 590.0 nM 6.23
CHEMBL4125982 — IC50 = 790.0 nM 6.10
CHEMBL4126535 — IC50 = 1100.0 nM 5.96
CHEMBL4129083 — IC50 = 1380.0 nM 5.86
CHEMBL4125794 — IC50 = 8510.0 nM 5.07
CHEMBL4127223 — IC50 = 8710.0 nM 5.06
CHEMBL4128202 — IC50 = 8910.0 nM 5.05
CHEMBL4128608 — IC50 = 33100.0 nM 4.48
CHEMBL4127845 — IC50 > 10000.0 nM -