PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

BSJ-04-175 is a potent, selective focal adhesion kinase (FAK, protein tyrosine kinase 2 or PTK2) inhibitor with biochemical IC50 of 22 nM, 30-fold selectivity over PYK2.

PF-719 (PF719) is a potent, selective Pyk2 inhibitor with IC50 of 17 nM, displays 25-fold selectvity over FAK (IC50=469 nM).

Y15 is a novel small molecule FAK phosphorylation inhibitor; specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK.

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation.

TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met.

PND-1186 is a potent FAK inhibitor with IC50 of 1.5 nM.

PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

PF-4618433 shows improved PYK2 potency, reduced p38 activity, and superior overall selectivity relative to the prototype BIRB796.

PF-431396 is dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor , PF-431396 has a Kd value of 445 nM for BRD4.

PF 573228 is a inhibitor of FAK with IC50 of 4 nM.

GSK2256098 is small molecule FAK kinase inhibitor.

Defactinib is a potent, selective, and orally active FAK inhibitor with demonstrated tolerability and preliminary clinical activity working as a single agent as well as in combination with paclitaxel.

YH-306 is a candidate drug in preventing growth and metastasis of colorectal cancer by modulating FAK signalling pathway.

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.

FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 (Compound B5) presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 (Compound B5) inhibits cell migration and invasion.

BJG-03-025 is a potent, highly selective FAK tyrosine kinase inhibitor with biochemical IC50 of 20.2 nM.BJG-03-025 demonstrates excellent kinome selectivity was profiled by KINOMEscan screening, PLK1 proved to be a false positive with IC50 of 8.3 uM, 100-300-fold selective for FAK.BJG-03-025 displays antiproliferative activity in three-dimensional (3D)-breast and gastric cancer models and impacts cellular signaling and migration.BJG-03-025 decreased phosphorylated FAK (pFAK Y397) in gastric cancer CDH1–/–RHOAY42C/+ organoid model, decreased aberrant signaling and proliferation of gastric cancer organoids.

FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.

AMP-945 is an inhibitor of the enzyme focal adhesion kinase (FAK).

CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma).

Defactinib is a potent, selective, and orally active FAK inhibitor with demonstrated tolerability and preliminary clinical activity working as a single agent as well as in combination with paclitaxel.

Petunidin chloride is an O-methylated anthocyanidin derived from delphinidin that imparts blue-red pigments to flowers, fruits, and red wine. Petunidin chloride binds with and suppresses the activity of focal adhesion kinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.

PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis.

NAMI-A is a ruthenium anticancer agent and a metastasis inhibitor.