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Assay Detail

CHEMBL5735331

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Binding
Inhibition Kinase Activity Assay: The FGFR1 inhibitory activities of compounds were measured based on their activity to inhibit phosphorylation of the biotinylated peptide (EGPWLEEEEEAYGWMDF; SEQ ID NO: 39) by a human FGFR1 enzyme. Phosphorylated biotinylated peptide was detected by time-resolved fluorometry using a europium cryptate-linked anti-phosphotyrosine antibody, and streptavidin linked to an allophycocyanin derivative, XL665. The half maximal inhibitory concentration (IC50) was calculated based on the inhibitory rate against the control group which does not contain the test substance.
ChEMBL ↗
213
Total Activities
71
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Fibroblast growth factor receptor 1 (CHEMBL3650) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

FGFR3 fusion gene and pharmaceutical drug targeting same
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 71 7.63 9.49
kon 71 - -
k_off 71 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3681271 — — 3 9.49
CHEMBL3681272 — — 3 9.17
CHEMBL3676325 — — 3 9.09
CHEMBL3681278 — — 3 8.85
CHEMBL3681240 — — 3 8.64
CHEMBL3676328 — — 3 8.57
CHEMBL3676315 — — 3 8.57
CHEMBL3681314 — — 3 8.54
CHEMBL3676316 — — 3 8.52
CHEMBL3907479 FGFR INHIBITOR DEBIO 1347 2.0 3 8.30
CHEMBL3681303 — — 3 8.26
CHEMBL3681270 — — 3 8.16
CHEMBL5847691 — — 3 8.10
CHEMBL5987182 — — 3 8.05
CHEMBL5953101 — — 3 8.02
CHEMBL3676324 — — 3 8.00
CHEMBL3681267 — — 3 7.96
CHEMBL3681274 — — 3 7.96
CHEMBL3676323 — — 3 7.82
CHEMBL3676331 — — 3 7.80
CHEMBL3676327 — — 3 7.77
CHEMBL3681247 — — 3 7.75
CHEMBL3681315 — — 3 7.68
CHEMBL3681250 — — 3 7.66
CHEMBL3681236 — — 3 7.66
CHEMBL3681248 — — 3 7.62
CHEMBL3681237 — — 3 7.60
CHEMBL3681316 — — 3 7.57
CHEMBL3681238 — — 3 7.54
CHEMBL3681298 — — 3 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3681271 — IC50 = 0.32 nM 9.49
CHEMBL3681272 — IC50 = 0.67 nM 9.17
CHEMBL3676325 — IC50 = 0.81 nM 9.09
CHEMBL3681278 — IC50 = 1.4 nM 8.85
CHEMBL3681240 — IC50 = 2.3 nM 8.64
CHEMBL3676328 — IC50 = 2.7 nM 8.57
CHEMBL3676315 — IC50 = 2.7 nM 8.57
CHEMBL3681314 — IC50 = 2.9 nM 8.54
CHEMBL3676316 — IC50 = 3.0 nM 8.52
CHEMBL3907479 FGFR INHIBITOR DEBIO 1347 IC50 = 5.0 nM 8.30
CHEMBL3681303 — IC50 = 5.5 nM 8.26
CHEMBL3681270 — IC50 = 6.9 nM 8.16
CHEMBL5847691 — IC50 = 7.9 nM 8.10
CHEMBL5987182 — IC50 = 9.0 nM 8.05
CHEMBL5953101 — IC50 = 9.6 nM 8.02
CHEMBL3676324 — IC50 = 10.0 nM 8.00
CHEMBL3681274 — IC50 = 11.0 nM 7.96
CHEMBL3681267 — IC50 = 11.0 nM 7.96
CHEMBL3676323 — IC50 = 15.0 nM 7.82
CHEMBL3676331 — IC50 = 16.0 nM 7.80
CHEMBL3676327 — IC50 = 17.0 nM 7.77
CHEMBL3681247 — IC50 = 18.0 nM 7.75
CHEMBL3681315 — IC50 = 21.0 nM 7.68
CHEMBL3681250 — IC50 = 22.0 nM 7.66
CHEMBL3681236 — IC50 = 22.0 nM 7.66
CHEMBL3681248 — IC50 = 24.0 nM 7.62
CHEMBL3681237 — IC50 = 25.0 nM 7.60
CHEMBL3681316 — IC50 = 27.0 nM 7.57
CHEMBL3681238 — IC50 = 29.0 nM 7.54
CHEMBL3676329 — IC50 = 30.0 nM 7.52
CHEMBL3681298 — IC50 = 30.0 nM 7.52
CHEMBL3676320 — IC50 = 30.0 nM 7.52
CHEMBL3676317 — IC50 = 31.0 nM 7.51
CHEMBL3681308 — IC50 = 31.0 nM 7.51
CHEMBL3681301 — IC50 = 33.0 nM 7.48
CHEMBL3681266 — IC50 = 33.0 nM 7.48
CHEMBL6044955 — IC50 = 35.0 nM 7.46
CHEMBL3681258 — IC50 = 36.0 nM 7.44
CHEMBL3681306 — IC50 = 38.0 nM 7.42
CHEMBL6024204 — IC50 = 38.0 nM 7.42
CHEMBL3681263 — IC50 = 39.0 nM 7.41
CHEMBL3681296 — IC50 = 40.0 nM 7.40
CHEMBL3676318 — IC50 = 42.0 nM 7.38
CHEMBL3676330 — IC50 = 42.0 nM 7.38
CHEMBL3681265 — IC50 = 43.0 nM 7.37
CHEMBL3676332 — IC50 = 43.0 nM 7.37
CHEMBL3681245 — IC50 = 43.0 nM 7.37
CHEMBL3681242 — IC50 = 45.0 nM 7.35
CHEMBL3681304 — IC50 = 46.0 nM 7.34
CHEMBL3681268 — IC50 = 48.0 nM 7.32