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Assay Detail

CHEMBL2155758

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Binding
Inhibition of JAK1
ChEMBL ↗
48
Total Activities
47
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase JAK1 (CHEMBL2835) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.
Kulagowski JJ, Blair W, Bull RJ, Chang C, Deshmukh G, Dyke HJ, Eigenbrot C, Ghilardi N, Gibbons P, Harrison TK, Hewitt PR, Liimatta M, Hurley CA, Johnson A, Johnson T, Kenny JR, Bir Kohli P, Maxey RJ, Mendonca R, Mortara K, Murray J, Narukulla R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Waszkowycz B, Zak M.
J Med Chem (2012) 55 : 5901 -5921
PubMed 22591402 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 47 8.02 9.40
IC50 1 8.00 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152300 — — 1 9.40
CHEMBL2152297 — — 1 9.30
CHEMBL2152401 — — 1 9.22
CHEMBL221959 TOFACITINIB 4.0 1 9.15
CHEMBL2152296 — — 2 9.05
CHEMBL2152398 — — 1 8.92
CHEMBL2152409 — — 1 8.77
CHEMBL2152307 — — 1 8.70
CHEMBL2152305 — — 1 8.62
CHEMBL2152422 — — 1 8.57
CHEMBL2152400 — — 1 8.54
CHEMBL2152424 — — 1 8.49
CHEMBL2152425 — — 1 8.43
CHEMBL2152420 — — 1 8.35
CHEMBL2152414 — — 1 8.24
CHEMBL2152421 — — 1 8.23
CHEMBL2152413 — — 1 8.21
CHEMBL2152412 — — 1 8.21
CHEMBL2152408 — — 1 8.08
CHEMBL2152419 — — 1 8.03
CHEMBL2152397 — — 1 8.02
CHEMBL2151053 — — 1 8.02
CHEMBL2152415 — — 1 8.01
CHEMBL1795071 RUXOLITINIB PHOSPHATE 4.0 1 8.00
CHEMBL2152418 — — 1 7.96
CHEMBL2152406 — — 1 7.96
CHEMBL2152299 — — 1 7.92
CHEMBL2152416 — — 1 7.92
CHEMBL2152423 — — 1 7.89
CHEMBL2152404 — — 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152300 — Ki = 0.4 nM 9.40
CHEMBL2152297 — Ki = 0.5 nM 9.30
CHEMBL2152401 — Ki = 0.6 nM 9.22
CHEMBL221959 TOFACITINIB Ki = 0.7 nM 9.15
CHEMBL2152296 — Ki = 0.9 nM 9.05
CHEMBL2152398 — Ki = 1.2 nM 8.92
CHEMBL2152409 — Ki = 1.7 nM 8.77
CHEMBL2152307 — Ki = 2.0 nM 8.70
CHEMBL2152296 — Ki = 2.2 nM 8.66
CHEMBL2152305 — Ki = 2.4 nM 8.62
CHEMBL2152422 — Ki = 2.7 nM 8.57
CHEMBL2152400 — Ki = 2.9 nM 8.54
CHEMBL2152424 — Ki = 3.2 nM 8.49
CHEMBL2152425 — Ki = 3.7 nM 8.43
CHEMBL2152420 — Ki = 4.5 nM 8.35
CHEMBL2152414 — Ki = 5.8 nM 8.24
CHEMBL2152421 — Ki = 5.9 nM 8.23
CHEMBL2152413 — Ki = 6.1 nM 8.21
CHEMBL2152412 — Ki = 6.1 nM 8.21
CHEMBL2152408 — Ki = 8.3 nM 8.08
CHEMBL2152419 — Ki = 9.3 nM 8.03
CHEMBL2152397 — Ki = 9.6 nM 8.02
CHEMBL2151053 — Ki = 9.5 nM 8.02
CHEMBL2152415 — Ki = 9.8 nM 8.01
CHEMBL1795071 RUXOLITINIB PHOSPHATE IC50 = 10.0 nM 8.00
CHEMBL2152418 — Ki = 11.0 nM 7.96
CHEMBL2152406 — Ki = 11.0 nM 7.96
CHEMBL2152299 — Ki = 12.0 nM 7.92
CHEMBL2152416 — Ki = 12.0 nM 7.92
CHEMBL2152423 — Ki = 13.0 nM 7.89
CHEMBL2152404 — Ki = 15.0 nM 7.82
CHEMBL2152303 — Ki = 15.0 nM 7.82
CHEMBL2152395 — Ki = 18.0 nM 7.75
CHEMBL2152394 — Ki = 19.0 nM 7.72
CHEMBL2152405 — Ki = 22.0 nM 7.66
CHEMBL2152301 — Ki = 24.0 nM 7.62
CHEMBL2152396 — Ki = 28.0 nM 7.55
CHEMBL2152402 — Ki = 32.0 nM 7.50
CHEMBL2152410 — Ki = 33.0 nM 7.48
CHEMBL2152403 — Ki = 43.0 nM 7.37
CHEMBL2152306 — Ki = 45.0 nM 7.35
CHEMBL2152399 — Ki = 50.0 nM 7.30
CHEMBL2152411 — Ki = 50.0 nM 7.30
CHEMBL2152304 — Ki = 62.0 nM 7.21
CHEMBL2152302 — Ki = 88.0 nM 7.06
CHEMBL2152407 — Ki = 96.0 nM 7.02
CHEMBL2152417 — Ki = 280.0 nM 6.55
CHEMBL2152298 — Ki = 610.0 nM 6.21