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Assay Detail

CHEMBL4622283

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Binding
Inhibition of human Notum (S81 to T451 residues) Cys330Ser mutant expressed in HEK293S GnTI cells using OPTS as substrate incubated for 40 mins by fluorescence based assay
ChEMBL ↗
84
Total Activities
84
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

Palmitoleoyl-protein carboxylesterase NOTUM (CHEMBL3714531) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Screening of a Custom-Designed Acid Fragment Library Identifies 1-Phenylpyrroles and 1-Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase Activity.
Mahy W, Patel M, Steadman D, Woodward HL, Atkinson BN, Svensson F, Willis NJ, Flint A, Papatheodorou D, Zhao Y, Vecchia L, Ruza RR, Hillier J, Frew S, Monaghan A, Costa A, Bictash M, Walter MW, Jones EY, Fish PV.
J Med Chem (2020) 63 : 9464 -9483
PubMed 32787107 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 84 5.52 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4637220 — — 1 6.96
CHEMBL4646852 — — 1 6.82
CHEMBL4639422 — — 1 6.70
CHEMBL4634413 — — 1 6.70
CHEMBL4646972 — — 1 6.66
CHEMBL4644041 — — 1 6.58
CHEMBL4645096 — — 1 6.57
CHEMBL4632764 — — 1 6.55
CHEMBL4634749 — — 1 6.44
CHEMBL4636171 — — 1 6.42
CHEMBL4632541 — — 1 6.39
CHEMBL4645532 — — 1 6.37
CHEMBL4645650 — — 1 6.37
CHEMBL4645103 — — 1 6.34
CHEMBL4638675 — — 1 6.24
CHEMBL4640525 — — 1 6.22
CHEMBL4646231 — — 1 6.20
CHEMBL4639509 — — 1 6.19
CHEMBL4632374 — — 1 6.10
CHEMBL4641069 — — 1 6.07
CHEMBL4648146 — — 1 6.07
CHEMBL4643261 — — 1 6.00
CHEMBL4646472 — — 1 5.92
CHEMBL4645641 — — 1 5.92
CHEMBL4639854 — — 1 5.89
CHEMBL4635656 — — 1 5.85
CHEMBL4644438 — — 1 5.82
CHEMBL3495655 — — 1 5.82
CHEMBL4637315 — — 1 5.82
CHEMBL4632861 — — 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4637220 — IC50 = 110.0 nM 6.96
CHEMBL4646852 — IC50 = 150.0 nM 6.82
CHEMBL4634413 — IC50 = 200.0 nM 6.70
CHEMBL4639422 — IC50 = 200.0 nM 6.70
CHEMBL4646972 — IC50 = 220.0 nM 6.66
CHEMBL4644041 — IC50 = 260.0 nM 6.58
CHEMBL4645096 — IC50 = 270.0 nM 6.57
CHEMBL4632764 — IC50 = 280.0 nM 6.55
CHEMBL4634749 — IC50 = 360.0 nM 6.44
CHEMBL4636171 — IC50 = 380.0 nM 6.42
CHEMBL4632541 — IC50 = 410.0 nM 6.39
CHEMBL4645532 — IC50 = 430.0 nM 6.37
CHEMBL4645650 — IC50 = 430.0 nM 6.37
CHEMBL4645103 — IC50 = 460.0 nM 6.34
CHEMBL4638675 — IC50 = 580.0 nM 6.24
CHEMBL4640525 — IC50 = 600.0 nM 6.22
CHEMBL4646231 — IC50 = 630.0 nM 6.20
CHEMBL4639509 — IC50 = 640.0 nM 6.19
CHEMBL4632374 — IC50 = 800.0 nM 6.10
CHEMBL4641069 — IC50 = 850.0 nM 6.07
CHEMBL4648146 — IC50 = 860.0 nM 6.07
CHEMBL4643261 — IC50 = 1000.0 nM 6.00
CHEMBL4646472 — IC50 = 1200.0 nM 5.92
CHEMBL4645641 — IC50 = 1200.0 nM 5.92
CHEMBL4639854 — IC50 = 1300.0 nM 5.89
CHEMBL4635656 — IC50 = 1400.0 nM 5.85
CHEMBL3495655 — IC50 = 1500.0 nM 5.82
CHEMBL4637315 — IC50 = 1500.0 nM 5.82
CHEMBL4632861 — IC50 = 1500.0 nM 5.82
CHEMBL4635705 — IC50 = 1500.0 nM 5.82
CHEMBL4644438 — IC50 = 1500.0 nM 5.82
CHEMBL4639496 — IC50 = 1700.0 nM 5.77
CHEMBL1329864 — IC50 = 1700.0 nM 5.77
CHEMBL2113925 — IC50 = 1900.0 nM 5.72
CHEMBL2113928 — IC50 = 2000.0 nM 5.70
CHEMBL4636423 — IC50 = 2000.0 nM 5.70
CHEMBL4647516 — IC50 = 2100.0 nM 5.68
CHEMBL4646239 — IC50 = 2200.0 nM 5.66
CHEMBL4646461 — IC50 = 2300.0 nM 5.64
CHEMBL4637428 — IC50 = 2300.0 nM 5.64
CHEMBL4644565 — IC50 = 2500.0 nM 5.60
CHEMBL4643979 — IC50 = 3100.0 nM 5.51
CHEMBL4636139 — IC50 = 3100.0 nM 5.51
CHEMBL4645998 — IC50 = 3100.0 nM 5.51
CHEMBL4640339 — IC50 = 3100.0 nM 5.51
CHEMBL4644737 — IC50 = 3300.0 nM 5.48
CHEMBL4632603 — IC50 = 3500.0 nM 5.46
CHEMBL4645808 — IC50 = 3800.0 nM 5.42
CHEMBL4642774 — IC50 = 4200.0 nM 5.38
CHEMBL1577069 — IC50 = 6300.0 nM 5.20