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Assay Detail

CHEMBL732617

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

Binding
Binding affinity for human recombinant Mitogen-activated protein kinase p38 in a fluorescent binding assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

MAP kinase p38 (CHEMBL2094115)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.
Regan J, Breitfelder S, Cirillo P, Gilmore T, Graham AG, Hickey E, Klaus B, Madwed J, Moriak M, Moss N, Pargellis C, Pav S, Proto A, Swinamer A, Tong L, Torcellini C.
J Med Chem (2002) 45 : 2994 -3008
PubMed 12086485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 44 7.28 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420047 1 9.00
CHEMBL84777 1 8.70
CHEMBL315100 1 8.52
CHEMBL86318 1 8.52
CHEMBL100847 1 8.52
CHEMBL314228 1 8.40
CHEMBL312873 1 8.30
CHEMBL314805 1 8.15
CHEMBL315059 1 8.10
CHEMBL85860 1 8.10
CHEMBL10 SB-203580 1 8.00
CHEMBL315023 1 7.92
CHEMBL314023 1 7.89
CHEMBL420231 1 7.85
CHEMBL85461 1 7.85
CHEMBL87224 1 7.72
CHEMBL314278 1 7.68
CHEMBL87289 1 7.66
CHEMBL87580 1 7.60
CHEMBL312895 1 7.51
CHEMBL84928 1 7.33
CHEMBL101035 1 7.06
CHEMBL86195 1 7.00
CHEMBL85942 1 6.89
CHEMBL85609 1 6.70
CHEMBL407173 1 6.58
CHEMBL83254 1 6.55
CHEMBL85985 1 6.50
CHEMBL88096 1 6.48
CHEMBL87277 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420047 Kd = 1.0 nM 9.00
CHEMBL84777 Kd = 2.0 nM 8.70
CHEMBL86318 Kd = 3.0 nM 8.52
CHEMBL100847 Kd = 3.0 nM 8.52
CHEMBL315100 Kd = 3.0 nM 8.52
CHEMBL314228 Kd = 4.0 nM 8.40
CHEMBL312873 Kd = 5.0 nM 8.30
CHEMBL314805 Kd = 7.0 nM 8.15
CHEMBL315059 Kd = 8.0 nM 8.10
CHEMBL85860 Kd = 8.0 nM 8.10
CHEMBL10 SB-203580 Kd = 10.0 nM 8.00
CHEMBL315023 Kd = 12.0 nM 7.92
CHEMBL314023 Kd = 13.0 nM 7.89
CHEMBL420231 Kd = 14.0 nM 7.85
CHEMBL85461 Kd = 14.0 nM 7.85
CHEMBL87224 Kd = 19.0 nM 7.72
CHEMBL314278 Kd = 21.0 nM 7.68
CHEMBL87289 Kd = 22.0 nM 7.66
CHEMBL87580 Kd = 25.0 nM 7.60
CHEMBL312895 Kd = 31.0 nM 7.51
CHEMBL84928 Kd = 47.0 nM 7.33
CHEMBL101035 Kd = 88.0 nM 7.06
CHEMBL86195 Kd = 100.0 nM 7.00
CHEMBL85942 Kd = 130.0 nM 6.89
CHEMBL85609 Kd = 200.0 nM 6.70
CHEMBL407173 Kd = 260.0 nM 6.58
CHEMBL83254 Kd = 280.0 nM 6.55
CHEMBL85985 Kd = 318.0 nM 6.50
CHEMBL88096 Kd = 330.0 nM 6.48
CHEMBL87277 Kd = 350.0 nM 6.46
CHEMBL313202 Kd = 400.0 nM 6.40
CHEMBL423862 Kd = 420.0 nM 6.38
CHEMBL87830 Kd = 500.0 nM 6.30
CHEMBL103676 Kd = 530.0 nM 6.28
CHEMBL87257 Kd = 760.0 nM 6.12
CHEMBL87018 Kd = 1200.0 nM 5.92
CHEMBL89154 Kd = 1400.0 nM 5.85
CHEMBL317876 Kd = 1500.0 nM 5.82
CHEMBL319681 Kd = 7500.0 nM 5.12
CHEMBL103275 Kd > 900.0 nM -
CHEMBL86962 Kd > 7000.0 nM -
CHEMBL313515 Kd > 7000.0 nM -
CHEMBL87610 Kd > 400.0 nM -
CHEMBL316570 Kd > 1000.0 nM -