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Assay Detail

CHEMBL678783

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

Binding
compound was tested for the ability to function as transport substrates for the human folate-binding protein(mFBP)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Folate receptor alpha (CHEMBL2121)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Protein structure-based design, synthesis, and biological evaluation of 5-thia-2,6-diamino-4(3H)-oxopyrimidines: potent inhibitors of glycinamide ribonucleotide transformylase with potent cell growth inhibition.
Varney MD, Palmer CL, Romines WH, Boritzki T, Margosiak SA, Almassy R, Janson CA, Bartlett C, Howland EJ, Ferre R.
J Med Chem (1997) 40 : 2502 -2524
PubMed 9258357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 8.66 9.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85871 1 9.81
CHEMBL84935 1 9.42
CHEMBL309415 1 9.24
CHEMBL82390 1 9.16
CHEMBL82261 1 9.02
CHEMBL85848 1 7.08
CHEMBL315627 1 6.87
CHEMBL84163 1 -
CHEMBL85436 1 -
CHEMBL315076 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85871 Kd = 0.153 nM 9.81
CHEMBL84935 Kd = 0.38 nM 9.42
CHEMBL309415 Kd = 0.57 nM 9.24
CHEMBL82390 Kd = 0.69 nM 9.16
CHEMBL82261 Kd = 0.95 nM 9.02
CHEMBL85848 Kd = 83.0 nM 7.08
CHEMBL315627 Kd = 136.0 nM 6.87
CHEMBL84163 Kd = 0.0032 nM -
CHEMBL85436 Kd = 0.0005 nM -
CHEMBL315076 Kd = 0.002 nM -