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Assay Detail

CHEMBL4843582

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

Binding
Inhibition of SF-tagged FAP (unknown origin) expressed in Drosophila S2 cells using fluorogenic substrate by spectrometric analysis
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type S2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prolyl endopeptidase FAP (CHEMBL4683)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship and biochemical evaluation of novel fibroblast activation protein and prolyl endopeptidase inhibitors with α-ketoamide warheads.
Šimková A, Ormsby T, Sidej N, Slavětínská LP, Brynda J, Beranová J, Šácha P, Majer P, Konvalinka J.
Eur J Med Chem (2021) 224 : 113717 -113717
PubMed 34371463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 8.80 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4877950 1 10.05
CHEMBL4878759 1 9.89
CHEMBL4864809 1 9.74
CHEMBL4853661 1 9.72
CHEMBL4850601 1 9.66
CHEMBL4876026 1 9.51
CHEMBL4868869 1 9.49
CHEMBL4850484 1 9.48
CHEMBL4867484 1 9.38
CHEMBL4873985 1 9.38
CHEMBL4864133 1 9.36
CHEMBL4854865 1 9.30
CHEMBL4871602 1 9.28
CHEMBL4855449 1 9.24
CHEMBL4859756 1 9.20
CHEMBL4868282 1 9.20
CHEMBL4863249 1 9.20
CHEMBL4847764 1 9.19
CHEMBL4851238 1 9.17
CHEMBL4855309 1 9.11
CHEMBL4846405 1 8.96
CHEMBL4870279 1 8.96
CHEMBL4870593 1 8.96
CHEMBL4871573 1 8.82
CHEMBL4861963 1 8.77
CHEMBL4869146 1 8.74
CHEMBL4864489 1 8.68
CHEMBL3233842 1 8.64
CHEMBL4872140 1 8.57
CHEMBL4850470 1 8.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4877950 IC50 = 0.089 nM 10.05
CHEMBL4878759 IC50 = 0.13 nM 9.89
CHEMBL4864809 IC50 = 0.18 nM 9.74
CHEMBL4853661 IC50 = 0.19 nM 9.72
CHEMBL4850601 IC50 = 0.22 nM 9.66
CHEMBL4876026 IC50 = 0.31 nM 9.51
CHEMBL4868869 IC50 = 0.32 nM 9.49
CHEMBL4850484 IC50 = 0.33 nM 9.48
CHEMBL4867484 IC50 = 0.42 nM 9.38
CHEMBL4873985 IC50 = 0.42 nM 9.38
CHEMBL4864133 IC50 = 0.44 nM 9.36
CHEMBL4854865 IC50 = 0.5 nM 9.30
CHEMBL4871602 IC50 = 0.53 nM 9.28
CHEMBL4855449 IC50 = 0.58 nM 9.24
CHEMBL4863249 IC50 = 0.63 nM 9.20
CHEMBL4859756 IC50 = 0.63 nM 9.20
CHEMBL4868282 IC50 = 0.63 nM 9.20
CHEMBL4847764 IC50 = 0.64 nM 9.19
CHEMBL4851238 IC50 = 0.67 nM 9.17
CHEMBL4855309 IC50 = 0.77 nM 9.11
CHEMBL4846405 IC50 = 1.1 nM 8.96
CHEMBL4870279 IC50 = 1.1 nM 8.96
CHEMBL4870593 IC50 = 1.1 nM 8.96
CHEMBL4871573 IC50 = 1.5 nM 8.82
CHEMBL4861963 IC50 = 1.7 nM 8.77
CHEMBL4869146 IC50 = 1.8 nM 8.74
CHEMBL4864489 IC50 = 2.1 nM 8.68
CHEMBL3233842 IC50 = 2.3 nM 8.64
CHEMBL4872140 IC50 = 2.7 nM 8.57
CHEMBL4850470 IC50 = 3.4 nM 8.47
CHEMBL4863606 IC50 = 3.7 nM 8.43
CHEMBL4870506 IC50 = 3.7 nM 8.43
CHEMBL4863090 IC50 = 4.0 nM 8.40
CHEMBL4875452 IC50 = 4.3 nM 8.37
CHEMBL4868792 IC50 = 5.0 nM 8.30
CHEMBL4874501 IC50 = 5.4 nM 8.27
CHEMBL4847560 IC50 = 6.7 nM 8.17
CHEMBL2385281 IC50 = 6.8 nM 8.17
CHEMBL4870027 IC50 = 7.2 nM 8.14
CHEMBL4863794 IC50 = 8.3 nM 8.08
CHEMBL4873662 IC50 = 11.0 nM 7.96
CHEMBL4874657 IC50 = 13.0 nM 7.89
CHEMBL4874659 IC50 = 15.0 nM 7.82
CHEMBL4861885 IC50 = 20.0 nM 7.70
CHEMBL4857711 IC50 = 24.0 nM 7.62
CHEMBL4869363 IC50 = 150.0 nM 6.82